Iminosulfonylurea dirivatives and herbicides

ABSTRACT

The present invention provides novel iminosulfonylurea derivatives which are useful as herbicides with excellent activity and selectivity. These derivatives can be used to protect rice, wheat, corn, soybean, cotton and sugar beet from weeds.

TECHNICAL FIELD

This application is a 371 of PCT/JP92/00808 filed Jun. 25, 1992.

The present invention relates to novel iminosulfonylurea derivatives,and herbicides containing them as active ingredients.

BACKGROUND TECHNIQUE

It is indispensable to use herbicides to protect important crop plantssuch as rice, wheat, corn, soybean, cotton and sugar beet from weeds andthereby to increase the harvest. Especially in recent years, a selectiveherbicide is desired which is capable of selectively killing weedswithout showing any phytotoxicity against crop plants when applied tothe foliages of crop plants and weeds simultaneously in a field wheresuch useful crop plants and weeds are coexistent. Further, with a viewto avoiding environmental pollution and reducing the costs fortransportation and application, researches and developments have beenconducted for many years for compounds having high herbicidal effects atlow doses. Some of the compounds having such properties are presentlyused as selective herbicides. However, there still exists a need forbetter new compounds having such properties.

As the prior art showing a chemical structure similar to that of thecompounds of the present invention, Japanese Unexamined PatentPublications No. 15962/1983, No. 103371/1983, No. 126859/1983, No.48973/1985, No. 214785/1985, No. 134377/1986, No. 151577/1989, No.45473/1990, No. 91060/1990, No. 7284/1991 and No. 68562/1991, and U.S.Pat. Nos. 4,559,081, 4,592,776, 4,602,939, 4,622,065, 4,666,508,4,696,695 and 4,741,762, disclose compounds having sulfonylurea bondedto a nitrogen atom. However, compounds having sulfonylurea bonded to anitrogen atom of an imino structure like the compounds of the presentinvention have not been known at all, and they are novel compounds.

DISCLOSURE OF THE INVENTION

The present inventors have conducted extensive researches over years todevelop selective herbicides for important crop plants and have studiedherbicidal properties of many compounds with an aim to find outcompounds having higher herbicidal activities as well as selectivity. Asa result, it has been found that an iminosulfonylurea derivative of theformula (1) or an agriculturally suitable salt thereof: ##STR1## whereinin Q1, Q2 and Q5, E is a sulfur atom, an oxygen atom or a nitrogen atommono-substituted by an optional substituent other than a hydrogen atom;in Q6, Q7 and Q8, J is a sulfur atom or an oxygen atom; in Q1 to Q8, anitrogen atom in the ring of Q is substituted by an optional substituentother than a hydrogen atom, and a carbon atom in the ring of Q may besubstituted by an optional substituent; and in Q9, the sulfur atom andthe nitrogen atom on the carbon atom to which the imino group of Q isbonded, are substituted by optional substituents other than hydrogenatoms, wherein Q is preferably ##STR2##

R^(a1) is a C₁₋₈ alkyl group, a C₃₋₇ cycloalkyl group, a C₁₋₆ alkylgroup substituted by a C₃₋₇ cycloalkyl group, a C₃₋₇ cycloalkenyl group,a C₁₋₆ alkyl group substituted by a C₃₋₇ cycloalkenyl group, a C₂₋₈alkenyl group, a C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by aC₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkenyloxygroup, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkynyloxy group, a C₁₋₆alkyl group substituted by a mono-, di- or poly-halogeno C₁₋₆ alkoxygroup, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogenoC₂₋₆ alkenyloxy group, a C₁₋₆ alkyl group substituted by a mono-, di- orpoly-halogeno C₂₋₆ alkynyloxy group, a C₁₋₆ alkyl group substituted by aC₁₋₆ alkylthio group, a C₁₋ 6 alkyl group substituted by a C₁₋₆alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆alkylsulfonyl group, a mono-, di- or poly-halogeno C₁₋₈ alkyl group, amono-, di- or poly-halogeno C₂₋₈ alkenyl group, a mono-, di- orpoly-halogeno C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by acyano group, a C₂₋₆ alkenyl group substituted by a cyano group, a C₂₋₆alkynyl group substituted by a cyano group, a C₁₋₆ alkyl groupsubstituted by a nitro group, a C₂₋₆ alkenyl group substituted by anitro group, a C₂₋₆ alkynyl group substituted by a nitro group, a C₁₋₆alkyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkenylgroup substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkynyl groupsubstituted by a C₂₋₇ alkoxycarbonyl group, a C₁₋₆ alkyl groupsubstituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl groupsubstituted by a mono-, di- or poly-halogeno C₂₋₇ alkylcarbonyl group, aC₁₋₆ alkyl group substituted by a C₃₋₇ alkenylcarbonyl group, a C₁₋₆alkyl group substituted by a C₃₋₇ alkynylcarbonyl group, a C₁₋₆ alkylgroup substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonylgroup substituted by a C₁₋₄ alkylthio group, a C₁₋₆ alkyl groupsubstituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₂₋₅alkylcarbonyl group substituted by a C₁₋₄ alkylsulfonyl group, a C₂₋₆alkenyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₂₋₆ alkynylgroup substituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl groupsubstituted by a C₁₋₆ alkylsulfamoyl group, a C₁₋₆ alkyl groupsubstituted by a C₁₋₆ alkoxysulfamoyl group, a C₁₋₆ alkyl groupsubstituted by a di(C₁₋₃ alkyl)sulfamoyl group, a C₁₋₆ alkyl groupsubstituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)sulfamoyl group, a C₁₋₆alkyl group substituted by a C₂₋₇ alkylcarbamoyl group, a C₁₋₆ alkylgroup substituted by a di(C₁₋₃ alkyl)carbamoyl group, a C₁₋₆ alkyl groupsubstituted by a C₂₋₇ alkoxycarbamoyl group, a C₁₋₆ alkyl groupsubstituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)carbamoyl group, a C₁₋₆alkyl group substituted by a C₁₋₆ alkylamino group, a C₁₋₆ alkyl groupsubstituted by a C₁₋₆ alkoxyamino group, a C₁₋₆ alkyl group substitutedby a di(C₁₋₃ alkyl)amino group, a C₁₋₆ alkyl group substituted by anN-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)amino group, a C₁₋₆ alkyl groupsubstituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆ alkyl)amino group, aC₁₋₆ alkyl group substituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆alkoxy)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₆alkylsulfonyl)-N-(C₁₋₆ alkyl)amino group, a C₁₋₆ alkyl group substitutedby an N-(C₁₋₆ alkylsulfonyl)-N-(C₁₋₆ alkoxy)amino group, a phenyl group(provided that such a phenyl group may be substituted by one or moresubstituents selected from the group consisting of a halogen atom, atrifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxygroup and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substitutedby a phenyl group (provided that such a phenyl group may be substitutedby one or more substituents selected from the group consisting of ahalogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkylgroup, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₂₋₇alkenyl group substituted by a phenyl group (provided that such a phenylgroup may be substituted by one or more substituents selected from thegroup consisting of a halogen atom, a trifluoromethyl group, a nitrogroup, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonylgroup), a C₂₋₆ alkynyl group substituted by a phenyl group (providedthat such a phenyl group may be substituted by one or more substituentsselected from the group consisting of a halogen atom, a trifluoromethylgroup, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenoxy group(provided that such a phenoxy group may be substituted by one or moresubstituents selected from the group consisting of a halogen atom, atrifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxygroup and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substitutedby a phenylthio group (provided that such a phenylthio group may besubstituted by one or more substituents selected from the groupconsisting of a halogen atom, a trifluoromethyl group, a nitro group, aC₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),a C₁₋₆ alkyl group substituted by a phenylsulfinyl group (provided thatsuch a phenylsulfinyl group may be substituted by one or moresubstituents selected from the group consisting of a halogen atom, atrifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxygroup and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substitutedby a phenylsulfonyl group (provided that such a phenylsulfonyl group maybe substituted by one or more substituents selected from the groupconsisting of a halogen atom, a trifluoromethyl group, a nitro group, aC₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),a C₁₋₆ alkyl group substituted by a benzyloxy group (provided that thephenyl group of such a benzyloxy group may be substituted by one or moresubstituents selected from the group consisting of a halogen atom, atrifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxygroup and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substitutedby a benzylthio group (provided that the phenyl group of such abenzylthio group may be substituted by one or more substituents selectedfrom the group consisting of a halogen atom, a trifluoromethyl group, anitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by abenzylsulfinyl group (provided that the phenyl group of such abenzylsulfinyl group may be substituted by one or more substituentsselected from the group consisting of a halogen atom, a trifluoromethylgroup, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by abenzylsulfonyl group (provided that the phenyl group of such abenzylsulfonyl group may be substituted by one or more substituentsselected from the group consisting of a halogen atom, a trifluoromethylgroup, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by aphenylcarbonyl group (provided that such a phenylcarbonyl group may besubstituted by one or more substituents selected from the groupconsisting of a halogen atom, a trifluoromethyl group, a nitro group, aC₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),a C₁₋₆ alkyl group substituted by a benzylcarbonyl group (provided thatthe phenyl group of such a benzylcarbonyl group may be substituted byone or more substituents selected from the group consisting of a halogenatom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl groupsubstituted by an amino group substituted by a C₁₋₄ alkylsulfonyl group,or a C₁₋₆ alkyl group substituted by an amino group substituted by aC₂₋₄ alkylcarbonyl group,

each of R^(a2) and R^(a3) which are independent of each other, is ahydrogen atom, a C₁₋₆ alkyl group, a mono-, di- or poly-halogeno C₁₋₆alkyl group, a C₁₋₆ alkoxy group, a mono-, di or poly-halogeno C₁₋₆alkoxy group, a C₁₋₆ alkylthio group, a C₁₋₆ alkylsulfinyl group, a C₁₋₆alkylsulfonyl group, a C₂₋₇ alkoxycarbonyl group, a C₂₋₇ alkylcarbonylgroup, a halogen atom, a nitro group, a cyano group, or a phenyl group(provided that such a phenyl group may be substituted by one or moresubstituents selected from the group consisting of a halogen atom, atrifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxygroup and a C₂₋₇ alkoxycarbonyl group),

each of R^(a4) and R^(a5) which are independent of each other, is ahydrogen atom, a C₁₋₈ alkyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynylgroup, or a phenyl group (provided that such a phenyl group may besubstituted by one or more substituents selected from the groupconsisting of a halogen atom, a trifluoromethyl group, a nitro group, aC₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),

R^(a6) is a C₁₋₈ alkyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynyl groupor a phenyl group (provided that such a phenyl group may be substitutedby one or more substituents selected from the group consisting of ahalogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkylgroup, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),

R^(b1) is a C₁₋₈ alkyl group, a C₃₋₇ cycloalkyl group, a C₁₋₆ alkylgroup substituted by a C₃₋₇ cycloalkyl group, a C₃₋₇ cycloalkenyl group,a C₁₋₆ alkyl group substituted by a C₃₋₇ cycloalkenyl group, a C₂₋₈alkenyl group, a C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by aC₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkenyloxygroup, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkynyloxy group, a C₁₋₆alkyl group substituted by a mono-, di or poly-halogeno C₁₋₆ alkoxygroup, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogenoC₂₋₆ alkenyloxy group, a C₁₋₆ alkyl group substituted by a mono-, di- orpoly-halogeno C₂₋₆ alkynyloxy group, a C₁₋₆ alkyl group substituted by aC₁₋₆ alkylthio group, a C₁₋₆ alkyl group substituted by a C₁₋₆alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆alkylsulfonyl group, a mono-, di- or poly-halogeno C₁₋₈ alkyl group, amono-, di- or poly-halogeno C₂₋₈ alkenyl group, a mono-, di- orpoly-halogeno C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by acyano group, a C₂₋₆ alkenyl group substituted by a cyano group, a C₂₋₆alkynyl group substituted by a cyano group, a C₁₋₆ alkyl groupsubstituted by a nitro group, a C₂₋₆ alkenyl group substituted by anitro group, a C₂₋₆ alkynyl group substituted by a nitro group, a C₁₋₆alkyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkenylgroup substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkynyl groupsubstituted by a C₂₋₇ alkoxycarbonyl group, a C₁₋₆ alkyl groupsubstituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl groupsubstituted by a mono-, di- or poly-halogeno C.sub. 2-7 alkylcarbonylgroup, a C₁₋₆ alkyl group substituted by a C₃₋₇ alkenylcarbonyl group, aC₁₋₆ alkyl group substituted by a C₃₋₇ alkynylcarbonyl group, a C₁₋₆alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by aC₁₋₄ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₅alkylcarbonyl group substituted by a C₁₋₄ alkylthio group, a C₁₋₆ alkylgroup substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₂₋₅alkylcarbonyl group substituted by a C₁₋₄ alkylsulfonyl group, a C₂₋₆alkenyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₂₋₆ alkynylgroup substituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl groupsubstituted by a C₁₋₆ alkylsulfamoyl group, a C₁₋₆ alkyl groupsubstituted by a C₁₋₆ alkoxysulfamoyl group, a C₁₋₆ alkyl groupsubstituted by a di(C₁₋₃ alkyl)sulfamoyl group, a C₁₋₆ alkyl groupsubstituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)sulfamoyl group, a C₁₋₆alkyl group substituted by a C₂₋₇ alkylcarbamoyl group, a C₁₋₆ alkylgroup substituted by a di(C₁₋₃ alkyl)carbamoyl group, a C₁₋₆ alkyl groupsubstituted by a C₂₋₇ alkoxycarbamoyl group, a C₁₋₆ alkyl groupsubstituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)carbamoyl group, a C₁₋₆alkyl group substituted by a C₁₋₆ alkylamino group, a C₁₋₆ alkyl groupsubstituted by a C₁₋₆ alkoxyamino group, a C₁₋₆ alkyl group substitutedby a di(C₁₋₃ alkyl)amino group, a C₁₋₆ alkyl group substituted by anN-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)amino group, a C₁₋₆ alkyl groupsubstituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆ alkyl)amino group, aC₁₋₆ alkyl group substituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆alkoxy)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₆alkylsulfonyl)-N-(C₁₋₆ alkyl)amino group, a C₁₋₆ alkyl group substitutedby an N-(C₁₋₆ alkylsulfonyl)-N-(C₁₋₆ alkoxy)amino group, a phenyl group(provided that such a phenyl group may be substituted by one or moresubstituents selected from the group consisting of a halogen atom, atrifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxygroup and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substitutedby a phenyl group (provided that such a phenyl group may be substitutedby one or more substituents selected from the group consisting of ahalogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkylgroup, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₂₋₇alkenyl group substituted by a phenyl group (provided that such a phenylgroup may be substituted by one or more substituents selected from thegroup consisting of a halogen atom, a trifluoromethyl group, a nitrogroup, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonylgroup), a C₂₋₆ alkynyl group substituted by a phenyl group (providedthat such a phenyl group may be substituted by one or more substituentsselected from the group consisting of a halogen atom, a trifluoromethylgroup, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenoxy group(provided that such a phenoxy group may be substituted by one or moresubstituents selected from the group consisting of a halogen atom, atrifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxygroup and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substitutedby a phenylthio group (provided that such a phenylthio group may besubstituted by one or more substituents selected from the groupconsisting of a halogen atom, a trifluoromethyl group, a nitro group, aC₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),a C₁₋₆ alkyl group substituted by a phenylsulfinyl group (provided thatsuch a phenylsulfinyl group may be substituted by one or moresubstituents selected from the group consisting of a halogen atom, atrifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxygroup and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substitutedby a phenylsulfonyl group (provided that such a phenylsulfonyl group maybe substituted by one or more substituents selected from the groupconsisting of a halogen atom, a trifluoromethyl group, a nitro group, aC₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),a C₁₋₆ alkyl group substituted by a benzyloxy group (provided that thephenyl group of such a benzyloxy group may be substituted by one or moresubstituents selected from the group consisting of a halogen atom, atrifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxygroup and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substitutedby a benzylthio group (provided that the phenyl group of such abenzylthio group may be substituted by one or more substituents selectedfrom the group consisting of a halogen atom, a trifluoromethyl group, anitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by abenzylsulfinyl group (provided that the phenyl group of such abenzylsulfinyl group may be substituted by one or more substituentsselected from the group consisting of a halogen atom, a trifluoromethylgroup, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by abenzylsulfonyl group (provided that the phenyl group of such abenzylsulfonyl group may be substituted by one or more substituentsselected from the group consisting of a halogen atom, a trifluoromethylgroup, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by aphenylcarbonyl group (provided that such a phenylcarbonyl group may besubstituted by one or more substituents selected from the groupconsisting of a halogen atom, a trifluoromethyl group, a nitro group, aC₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),a C₁₋₆ alkyl group substituted by a benzylcarbonyl group (provided thatthe phenyl group of such a benzylcarbonyl group may be substituted byone or more substituents selected from the group consisting of a halogenatom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl groupsubstituted by an amino group substituted by a C₁₋₄ alkylsulfonyl group,or a C₁₋₆ alkyl group substituted by an amino group substituted by aC₂₋₄ alkylcarbonyl group,

R^(b2) is a hydrogen atom, a C₁₋₆ alkyl group, a mono-, di- orpoly-halogeno C₁₋₆ alkyl group, a C₁₋₆ alkoxy group, a mono-, di- orpoly-halogeno C₁₋₆ alkoxy group, a C₁₋₆ alkylthio group, a C₁₋₆alkylsulfinyl group, a C₁₋₆ alkylsulfonyl group, a C₂₋₇ alkoxycarbonylgroup, a C₂₋₇ alkylcarbonyl group, a halogen atom, a nitro group, acyano group, or a phenyl group (provided that such a phenyl group may besubstituted by one or more substituents selected from the groupconsisting of a halogen atom, a trifluoromethyl group, a nitro group, aC₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),

R^(b3) is a C₁₋₆ alkyl group, a C₂₋₆ alkenyl group or a C₂₋₆ alkynylgroup,

R^(b4) is a hydrogen atom, or a C₁₋₆ alkyl group,

R^(b5) is a hydrogen atom, or a C₁₋₆ alkyl group,

R^(c1) is a C₁₋₈ alkyl group, a C₃₋₇ cycloalkyl group, a C₁₋₆ alkylgroup substituted by a C₃₋₇ cycloalkyl group, a C₃₋₇ cycloalkenyl group,a C₁₋₆ alkyl group substituted by a C₃₋₇ cycloalkenyl group, a C₂₋₈alkenyl group, a C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by aC₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkenyloxygroup, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkynyloxy group, a C₁₋₆alkyl group substituted by a mono-, di- or poly-halogeno C₁₋₆ alkoxygroup, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogenoC₂₋₆ alkenyloxy group, a C₁₋₆ alkyl group substituted by a mono-, di- orpoly-halogeno C₂₋₆ alkynyloxy group, a C₁₋₆ alkyl group substituted by aC₁₋₆ alkylthio group, a C₁₋₆ alkyl group substituted by a C₁₋₆alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆alkylsulfonyl group, a mono-, di- or poly-halogeno C₁₋₈ alkyl group, amono-, di- or poly-halogeno C₂₋₈ alkenyl group, a mono-, di- orpoly-halogeno C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by acyano group, a C₂₋₆ alkenyl group substituted by a cyano group, a C₂₋₆alkynyl group substituted by a cyano group, a C₁₋₆ alkyl groupsubstituted by a nitro group, a C₂₋₆ alkenyl group substituted by anitro group, a C₂₋₆ alkynyl group substituted by a nitro group, a C₁₋₆alkyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkenylgroup substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkynyl groupsubstituted by a C₂₋₇ alkoxycarbonyl group, a C₁₋₆ alkyl groupsubstituted by a C₂₋₇ alkylcarbonyl group, a C.sub. 1-6 alkyl groupsubstituted by a mono-, di- or poly-halogeno C₂₋₇ alkylcarbonyl group, aC₁₋₆ alkyl group substituted by a C₃₋₇ alkenylcarbonyl group, a C₁₋₆alkyl group substituted by a C₃₋₇ alkynylcarbonyl group, a C₁₋₆ alkylgroup substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonylgroup substituted by a C₁₋₄ alkylthio group, a C₁₋₆ alkyl groupsubstituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₂₋₅alkylcarbonyl group substituted by a C₁₋₄ alkylsulfonyl group, a C₂₋₆alkenyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₂₋₆ alkynylgroup substituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl groupsubstituted by a C₁₋₆ alkylsulfamoyl group, a C₁₋₆ alkyl groupsubstituted by a C₁₋₆ alkoxysulfamoyl group, a C₁₋₆ alkyl groupsubstituted by a di(C₁₋₃ alkyl)sulfamoyl group, a C₁₋₆ alkyl groupsubstituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)sulfamoyl group, a C₁₋₆alkyl group substituted by a C₂₋₇ alkylcarbamoyl group, a C₁₋₆ alkylgroup substituted by a di(C₁₋₃ alkyl)carbamoyl group, a C₁₋₆ alkyl groupsubstituted by a C₂₋₇ alkoxycarbamoyl group, a C₁₋₆ alkyl groupsubstituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)carbamoyl group, a C₁₋₆alkyl group substituted by a C₁₋₆ alkylamino group, a C₁₋₆ alkyl groupsubstituted by a C₁₋₆ alkoxyamino group, a C₁₋₆ alkyl group substitutedby a di(C₁₋₃ alkyl)amino group, a C₁₋₆ alkyl group substituted by anN-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)amino group, a C₁₋₆ alkyl groupsubstituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆ alkyl)amino group, aC₁₋₆ alkyl group substituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆alkoxy)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₆alkylsulfonyl)-N-(C₁₋₆ alkyl)amino group, a C₁₋₆ alkyl group substitutedby an N-(C₁₋₆ alkylsulfonyl)-N-(C₁₋₆ alkoxy)amino group, a phenyl group(provided that such a phenyl group may be substituted by one or moresubstituents selected from the group consisting of a halogen atom, atrifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxygroup and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substitutedby a phenyl group (provided that such a phenyl group may be substitutedby one or more substituents selected from the group consisting of ahalogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkylgroup, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₂₋₇alkenyl group substituted by a phenyl group (provided that such a phenylgroup may be substituted by one or more substituents selected from thegroup consisting of a halogen atom, a trifluoromethyl group, a nitrogroup, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonylgroup), a C₂₋₆ alkynyl group substituted by a phenyl group (providedthat such a phenyl group may be substituted by one or more substituentsselected from the group consisting of a halogen atom, a trifluoromethylgroup, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenoxy group(provided that such a phenoxy group may be substituted by one or moresubstituents selected from the group consisting of a halogen atom, atrifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxygroup and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substitutedby a phenylthio group (provided that such a phenylthio group may besubstituted by one or more substituents selected from the groupconsisting of a halogen atom, a trifluoromethyl group, a nitro group, aC₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),a C₁₋₆ alkyl group substituted by a phenylsulfinyl group (provided thatsuch a phenylsulfinyl group may be substituted by one or moresubstituents selected from the group consisting of a halogen atom, atrifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxygroup and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substitutedby a phenylsulfonyl group (provided that such a phenylsulfonyl group maybe substituted by one or more substituents selected from the groupconsisting of a halogen atom, a trifluoromethyl group, a nitro group, aC₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),a C₁₋₆ alkyl group substituted by a benzyloxy group (provided that thephenyl group of such a benzyloxy group may be substituted by one or moresubstituents selected from the group consisting of a halogen atom, atrifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxygroup and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substitutedby a benzylthio group (provided that the phenyl group of such abenzylthio group may be substituted by one or more substituents selectedfrom the group consisting of a halogen atom, a trifluoromethyl group, anitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by abenzylsulfinyl group (provided that the phenyl group of such abenzylsulfinyl group may be substituted by one or more substituentsselected from the group consisting of a halogen atom, a trifluoromethylgroup, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by abenzylsulfonyl group (provided that the phenyl group of such abenzylsulfonyl group may be substituted by one or more substituentsselected from the group consisting of a halogen atom, a trifluoromethylgroup, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by aphenylcarbonyl group (provided that such a phenylcarbonyl group may besubstituted by one or more substituents selected from the groupconsisting of a halogen atom, a trifluoromethyl group, a nitro group, aC₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),a C₁₋₆ alkyl group substituted by a benzylcarbonyl group (provided thatthe phenyl group of such a benzylcarbonyl group may be substituted byone or more substituents selected from the group consisting of a halogenatom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl groupsubstituted by an amino group substituted by a C₁₋₄ alkylsulfonyl group,or a C₁₋₆ alkyl group substituted by an amino group substituted by aC₂₋₄ alkylcarbonyl group,

each of R^(c2), R^(c3), R^(c4), R^(c5), R^(c6), R^(c11) and R^(c12)which are independent of one another, is a hydrogen atom, a C₁₋₈ alkylgroup, a C₂₋₈ alkenyl group, a C₂₋₈ alkynyl group, or a phenyl group(provided that such a phenyl group may be substituted by one or moresubstituents selected from the group consisting of a halogen atom, atrifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxygroup and a C₂₋₇ alkoxycarbonyl group),

each of R^(c7), R^(c8), R^(c9), R^(c10), R^(c13) and R^(c14) which areindependent of one another, is a hydrogen atom, a C₁₋₆ alkyl group, amono-, di- or poly-halogeno C₁₋₆ alkyl group, a C₁₋₆ alkoxy group, amono, di- or poly-halogeno C₁₋₆ alkoxy group, a C₁₋₆ alkylthio group, aC₁₋₆ alkylsulfinyl group, a C₁₋₆ alkylsulfonyl group, a C₂₋₇alkoxycarbonyl group, a C₂₋₇ alkylcarbonyl group, a halogen atom, anitro group, a cyano group, or a phenyl group (provided that such aphenyl group may be substituted by one or more substituents selectedfrom the group consisting of a halogen atom, a trifluoromethyl group, anitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group),

R^(d1) is a C₁₋₈ alkyl group, a C₃₋₇ cycloalkyl group, a C₁₋₆ alkylgroup substituted by a C₃₋₇ cycloalkyl group, a C₃₋₇ cycloalkenyl group,a C₁₋₆ alkyl group substituted by a C₃₋₇ cycloalkenyl group, a C₂₋₈alkenyl group, a C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by aC₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkenyloxygroup, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkynyloxy group, a C₁₋₆alkyl group substituted by a mono-, di or poly-halogeno C₁₋₆ alkoxygroup, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogenoC₂₋₆ alkenyloxy group, a C₁₋₆ alkyl group substituted by a mono-, di- orpoly-halogeno C₂₋₆ alkynyloxy group, a C₁₋₆ alkyl group substituted by aC₁₋₆ alkylthio group, a C₁₋₆ alkyl group substituted by a C₁₋₆alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆alkylsulfonyl group, a mono-, di- or poly-halogeno C₁₋₈ alkyl group, amono-, di- or poly-halogeno C₂₋₈ alkenyl group, a mono-, di- orpoly-halogeno C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by acyano group, a C₂₋₆ alkenyl group substituted by a cyano group, a C₂₋₆alkynyl group substituted by a cyano group, a C₁₋₆ alkyl groupsubstituted by a nitro group, a C₂₋₆ alkenyl group substituted by anitro group, a C₂₋₆ alkynyl group substituted by a nitro group, a C₁₋₆alkyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkenylgroup substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkynyl groupsubstituted by a C₂₋₇ alkoxycarbonyl group, a C₁₋₆ alkyl groupsubstituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl groupsubstituted by a mono-, di- or poly-halogeno C₂₋₇ alkylcarbonyl group, aC₁₋₆ alkyl group substituted by a C₃₋₇ alkenylcarbonyl group, a C₁₋₆alkyl group substituted by a C₃₋₇ alkynylcarbonyl group, a C₁₋₆ alkylgroup substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonylgroup substituted by a C₁₋₄ alkylthio group, a C₁₋₆ alkyl groupsubstituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₂₋₅alkylcarbonyl group substituted by a C₁₋₄ alkylsulfonyl group, a C₂₋₆alkenyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₂₋₆ alkynylgroup substituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl groupsubstituted by a C₁₋₆ alkylsulfamoyl group, a C₁₋₆ alkyl groupsubstituted by a C₁₋₆ alkoxysulfamoyl group, a C₁₋₆ alkyl groupsubstituted by a di(C₁₋₃ alkyl)sulfamoyl group, a C₁₋₆ alkyl groupsubstituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)sulfamoyl group, a C₁₋₆alkyl group substituted by a C₂₋₇ alkylcarbamoyl group, a C₁₋₆ alkylgroup substituted by a di(C₁₋₃ alkyl)carbamoyl group, a C₁₋₆ alkyl groupsubstituted by a C₂₋₇ alkoxycarbamoyl group, a C₁₋₆ alkyl groupsubstituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)carbamoyl group, a C₁₋₆alkyl group substituted by a C₁₋₆ alkylamino group, a C₁₋₆ alkyl groupsubstituted by a C₁₋₆ alkoxyamino group, a C₁₋₆ alkyl group substitutedby a di(C₁₋₃ alkyl)amino group, a C₁₋₆ alkyl group substituted by anN-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)amino group, a C₁₋₆ alkyl groupsubstituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆ alkyl)amino group, aC₁₋₆ alkyl group substituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆alkoxy)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₆alkylsulfonyl)-N-(C.sub. 1-6 alkyl)amino group, a C₁₋₆ alkyl groupsubstituted by an N-(C₁₋₆ alkylsulfonyl)-N-(C₁₋₆ alkoxy)amino group, aphenyl group (provided that such a phenyl group may be substituted byone or more substituents selected from the group consisting of a halogenatom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl groupsubstituted by a phenyl group (provided that such a phenyl group may besubstituted by one or more substituents selected from the groupconsisting of a halogen atom, a trifluoromethyl group, a nitro group, aC₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),a C₂₋₇ alkenyl group substituted by a phenyl group (provided that such aphenyl group may be substituted by one or more substituents selectedfrom the group consisting of a halogen atom, a trifluoromethyl group, anitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₂₋₆ alkynyl group substituted by a phenylgroup (provided that such a phenyl group may be substituted by one ormore substituents selected from the group consisting of a halogen atom,a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl groupsubstituted by a phenoxy group (provided that such a phenoxy group maybe substituted by one or more substituents selected from the groupconsisting of a halogen atom, a trifluoromethyl group, a nitro group, aC₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),a C₁₋₆ alkyl group substituted by a phenylthio group (provided that sucha phenylthio group may be substituted by one or more substituentsselected from the group consisting of a halogen atom, a trifluoromethylgroup, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by aphenylsulfinyl group (provided that such a phenylsulfinyl group may besubstituted by one or more substituents selected from the groupconsisting of a halogen atom, a trifluoromethyl group, a nitro group, aC₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),a C₁₋₆ alkyl group substituted by a phenylsulfonyl group (provided thatsuch a phenylsulfonyl group may be substituted by one or moresubstituents selected from the group consisting of a halogen atom, atrifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxygroup and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substitutedby a benzyloxy group (provided that the phenyl group of such a benzyloxygroup may be substituted by one or more substituents selected from thegroup consisting of a halogen atom, a trifluoromethyl group, a nitrogroup, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonylgroup), a C₁₋₆ alkyl group substituted by a benzylthio group (providedthat the phenyl group of such a benzylthio group may be substituted byone or more substituents selected from the group consisting of a halogenatom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl groupsubstituted by a benzylsulfinyl group (provided that the phenyl group ofsuch a benzylsulfinyl group may be substituted by one or moresubstituents selected from the group consisting of a halogen atom, atrifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxygroup and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substitutedby a benzylsulfonyl group (provided that the phenyl group of such abenzylsulfonyl group may be substituted by one or more substituentsselected from the group consisting of a halogen atom, a trifluoromethylgroup, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by aphenylcarbonyl group (provided that such a phenylcarbonyl group may besubstituted by one or more substituents selected from the groupconsisting of a halogen atom, a trifluoromethyl group, a nitro group, aC₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),a C₁₋₆ alkyl group substituted by a benzylcarbonyl group (provided thatthe phenyl group of such a benzylcarbonyl group may be substituted byone or more substituents selected from the group consisting of a halogenatom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl groupsubstituted by an amino group substituted by a C₁₋₄ alkylsulfonyl group,or a C₁₋₆ alkyl group substituted by an amino group substituted by aC₂₋₄ alkylcarbonyl group,

each of R^(d2), R^(d3) and R^(d4) which are independent of one another,is a hydrogen atom, a C₁₋₈ alkyl group, a C₂₋₈ alkenyl group, a C₂₋₈alkynyl group, or a phenyl group (provided that such a phenyl group maybe substituted by one or more substituents selected from the groupconsisting of a halogen atom, a trifluoromethyl group, a nitro group, aC₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),

R^(d5) is a C₁₋₈ alkyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynylgroup, or a phenyl group (provided that such a phenyl group may besubstituted by one or more substituents selected from the groupconsisting of a halogen atom, a trifluoromethyl group, a nitro group, aC₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),

R^(d6) is a C₁₋₈ alkyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynylgroup, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylthio group, a C₁₋₆alkyl group substituted by a C₁₋₆ alkylsulfinyl group, a C₁₋₆ alkylgroup substituted by a C₁₋₆ alkylsulfonyl group, a C₁₋₆ alkyl groupsubstituted by a C₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by aC₂₋₇ alkoxycarbonyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a cyano group, aphenyl group (provided that such a phenyl group may be substituted byone or more substituents selected from the group consisting of a halogenatom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆alkoxy group and a C₂₋₇ alkoxycarbonyl group), or a C₁₋₆ alkyl groupsubstituted by a phenyl group (provided that such a phenyl group may besubstituted by one or more substituents selected from the groupconsisting of a halogen atom, a trifluoromethyl group, a nitro group, aC₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),

R^(e1) is a C₁₋₈ alkyl group, a C₃₋₇ cycloalkyl group, a C₁₋₆ alkylgroup substituted by a C₃₋₇ cycloalkyl group, a C₃₋₇ cycloalkenyl group,a C₁₋₆ alkyl group substituted by a C₃₋₇ cycloalkenyl group, a C₂₋₈alkenyl group, a C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by aC₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkenyloxygroup, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkynyloxy group, a C₁₋₆alkyl group substituted by a mono-, di- or poly-halogeno C₁₋₆ alkoxygroup, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogenoC₂₋₆ alkenyloxy group, a C₁₋₆ alkyl group substituted by a mono-, di- orpoly-halogeno C₂₋₆ alkynyloxy group, a C₁₋₆ alkyl group substituted by aC₁₋₆ alkylthio group, a C₁₋₆ alkyl group substituted by a C₁₋₆alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆alkylsulfonyl group, a mono-, di- or poly-halogeno C₁₋₈ alkyl group, amono-, di- or poly-halogeno C₂₋₈ alkenyl group, a mono-, di- orpoly-halogeno C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by acyano group, a C₂₋₆ alkenyl group substituted by a cyano group, a C₂₋₆alkynyl group substituted by a cyano group, a C₁₋₆ alkyl groupsubstituted by a nitro group, a C₂₋₆ alkenyl group substituted by anitro group, a C₂₋₆ alkynyl group substituted by a nitro group, a C₁₋₆alkyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkenylgroup substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkynyl groupsubstituted by a C₂₋₇ alkoxycarbonyl group, a C₁₋₆ alkyl groupsubstituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl groupsubstituted by a mono-, di- or poly-halogeno C.sub. 2-7 alkylcarbonylgroup, a C₁₋₆ alkyl group substituted by a C₃₋₇ alkenylcarbonyl group, aC₁₋₆ alkyl group substituted by a C₃₋₇ alkynylcarbonyl group, a C₁₋₆alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by aC₁₋₄ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₅alkylcarbonyl group substituted by a C₁₋₄ alkylthio group, a C₁₋₆ alkylgroup substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₂₋₅alkylcarbonyl group substituted by a C₁₋₄ alkylsulfonyl group, a C₂₋₆alkenyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₂₋₆ alkynylgroup substituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl groupsubstituted by a C₁₋₆ alkylsulfamoyl group, a C₁₋₆ alkyl groupsubstituted by a C₁₋₆ alkoxysulfamoyl group, a C₁₋₆ alkyl groupsubstituted by a di(C₁₋₃ alkyl)sulfamoyl group, a C₁₋₆ alkyl groupsubstituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)sulfamoyl group, a C₁₋₆alkyl group substituted by a C₂₋₇ alkylcarbamoyl group, a C₁₋₆ alkylgroup substituted by a di(C₁₋₃ alkyl)carbamoyl group, a C₁₋₆ alkyl groupsubstituted by a C₂₋₇ alkoxycarbamoyl group, a C₁₋₆ alkyl groupsubstituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)carbamoyl group, a C₁₋₆alkyl group substituted by a C₁₋₆ alkylamino group, a C₁₋₆ alkyl groupsubstituted by a C₁₋₆ alkoxyamino group, a C₁₋₆ alkyl group substitutedby a di(C₁₋₃ alkyl)amino group, a C₁₋₆ alkyl group substituted by anN-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)amino group, a C₁₋₆ alkyl groupsubstituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆ alkyl)amino group, aC₁₋₆ alkyl group substituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆alkoxy)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₆alkylsulfonyl)-N-(C₁₋₆ alkyl)amino group, a C₁₋₆ alkyl group substitutedby an N-(C₁₋₆ alkylsulfonyl)-N-(C₁₋₆ alkoxy)amino group, a phenyl group(provided that such a phenyl group may be substituted by one or moresubstituents selected from the group consisting of a halogen atom, atrifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxygroup and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substitutedby a phenyl group (provided that such a phenyl group may be substitutedby one or more substituents selected from the group consisting of ahalogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkylgroup, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₂₋₇alkenyl group substituted by a phenyl group (provided that such a phenylgroup may be substituted by one or more substituents selected from thegroup consisting of a halogen atom, a trifluoromethyl group, a nitrogroup, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonylgroup), a C₂₋₆ alkynyl group substituted by a phenyl group (providedthat such a phenyl group may be substituted by one or more substituentsselected from the group consisting of a halogen atom, a trifluoromethylgroup, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenoxy group(provided that such a phenoxy group may be substituted by one or moresubstituents selected from the group consisting of a halogen atom, atrifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxygroup and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substitutedby a phenylthio group (provided that such a phenylthio group may besubstituted by one or more substituents selected from the groupconsisting of a halogen atom, a trifluoromethyl group, a nitro group, aC₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),a C₁₋₆ alkyl group substituted by a phenylsulfinyl group (provided thatsuch a phenylsulfinyl group may be substituted by one or moresubstituents selected from the group consisting of a halogen atom, atrifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxygroup and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substitutedby a phenylsulfonyl group (provided that such a phenylsulfonyl group maybe substituted by one or more substituents selected from the groupconsisting of a halogen atom, a trifluoromethyl group, a nitro group, aC₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),a C₁₋₆ alkyl group substituted by a benzyloxy group (provided that thephenyl group of such a benzyloxy group may be substituted by one or moresubstituents selected from the group consisting of a halogen atom, atrifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxygroup and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substitutedby a benzylthio group (provided that the phenyl group of such abenzylthio group may be substituted by one or more substituents selectedfrom the group consisting of a halogen atom, a trifluoromethyl group, anitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by abenzylsulfinyl group (provided that the phenyl group of such abenzylsulfinyl group may be substituted by one or more substituentsselected from the group consisting of a halogen atom, a trifluoromethylgroup, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by abenzylsulfonyl group (provided that the phenyl group of such abenzylsulfonyl group may be substituted by one or more substituentsselected from the group consisting of a halogen atom, a trifluoromethylgroup, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by aphenylcarbonyl group (provided that such a phenylcarbonyl group may besubstituted by one or more substituents selected from the groupconsisting of a halogen atom, a trifluoromethyl group, a nitro group, aC₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),a C₁₋₆ alkyl group substituted by a benzylcarbonyl group (provided thatthe phenyl group of such a benzylcarbonyl group may be substituted byone or more substituents selected from the group consisting of a halogenatom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl groupsubstituted by an amino group substituted by a C₁₋₄ alkylsulfonyl group,or a C₁₋₆ alkyl group substituted by an amino group substituted by aC₂₋₄ alkylcarbonyl group,

each of R^(e2), R^(e3), R^(e6) and R^(e7) which are independent of oneanother, is a hydrogen atom, a C₁₋₆ alkyl group, a mono-, di- orpoly-halogeno C₁₋₆ alkyl group, a C₁₋₆ alkoxy group, a mono-, di- orpoly-halogeno C₁₋₆ alkoxy group, a C₁₋₆ alkylthio group, a C₁₋₆alkylsulfinyl group, a C₁₋₆ alkylsulfonyl group, a C₂₋₇ alkoxycarbonylgroup, a C₂₋₇ alkylcarbonyl group, a halogen atom, a nitro group, acyano group, or a phenyl group (provided that such a phenyl group may besubstituted by one or more substituents selected from the groupconsisting of a halogen atom, a trifluoromethyl group, a nitro group, aC₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),

each of R^(e4), R^(e5), R^(e8), R^(e9) and R^(e10) which are independentof one another, is a hydrogen atom, a C₁₋₈ alkyl group, a C₂₋₈ alkenylgroup, a C₂₋₈ alkynyl group, or a phenyl group (provided that such aphenyl group may be substituted by one or more substituents selectedfrom the group consisting of a halogen atom, a trifluoromethyl group, anitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group),

R^(f1) is a C₁₋₈ alkyl group, a C₃₋₇ cycloalkyl group, a C₁₋₆ alkylgroup substituted by a C₃₋₇ cycloalkyl group, a C₃₋₇ cycloalkenyl group,a C₁₋₆ alkyl group substituted by a C₃₋₇ cycloalkenyl group, a C₂₋₈alkenyl group, a C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by aC₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkenyloxygroup, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkynyloxy group, a C₁₋₆alkyl group substituted by a mono-, di- or poly-halogeno C₁₋₆ alkoxygroup, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogenoC₂₋₆ alkenyloxy group, a C₁₋₆ alkyl group substituted by a mono-, di- orpoly-halogeno C₂₋₆ alkynyloxy group, a C₁₋₆ alkyl group substituted by aC₁₋₆ alkylthio group, a C₁₋₆ alkyl group substituted by a C₁₋₆alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆alkylsulfonyl group, a mono-, di- or poly-halogeno C₁₋₈ alkyl group, amono-, di- or poly-halogeno C₂₋₈ alkenyl group, a mono-, di- orpoly-halogeno C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by acyano group, a C₂₋₆ alkenyl group substituted by a cyano group, a C₂₋₆alkynyl group substituted by a cyano group, a C₁₋₆ alkyl groupsubstituted by a nitro group, a C₂₋₆ alkenyl group substituted by anitro group, a C₂₋₆ alkynyl group substituted by a nitro group, a C₁₋₆alkyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkenylgroup substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkynyl groupsubstituted by a C₂₋₇ alkoxycarbonyl group, a C₁₋₆ alkyl groupsubstituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl groupsubstituted by a mono-, di- or poly-halogeno C₂₋₇ alkylcarbonyl group, aC₁₋₆ alkyl group substituted by a C₃₋₇ alkenylcarbonyl group, a C₁₋₆alkyl group substituted by a C₃₋₇ alkynylcarbonyl group, a C₁₋₆ alkylgroup substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonylgroup substituted by a C₁₋₄ alkylthio group, a C₁₋₆ alkyl groupsubstituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₂₋₅alkylcarbonyl group substituted by a C₁₋₄ alkylsulfonyl group, a C₂₋₆alkenyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₂₋₆ alkynylgroup substituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl groupsubstituted by a C₁₋₆ alkylsulfamoyl group, a C₁₋₆ alkyl groupsubstituted by a C₁₋₆ alkoxysulfamoyl group, a C₁₋₆ alkyl groupsubstituted by a di(C₁₋₃ alkyl)sulfamoyl group, a C₁₋₆ alkyl groupsubstituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)sulfamoyl group, a C₁₋₆alkyl group substituted by a C₂₋₇ alkylcarbamoyl group, a C₁₋₆ alkylgroup substituted by a di(C₁₋₃ alkyl)carbamoyl group, a C₁₋₆ alkyl groupsubstituted by a C₂₋₇ alkoxycarbamoyl group, a C₁₋₆ alkyl groupsubstituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)carbamoyl group, a C₁₋₆alkyl group substituted by a C₁₋₆ alkylamino group, a C₁₋₆ alkyl groupsubstituted by a C₁₋₆ alkoxyamino group, a C₁₋₆ alkyl group substitutedby a di(C₁₋₃ alkyl)amino group, a C₁₋₆ alkyl group substituted by anN-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)amino group, a C₁₋₆ alkyl groupsubstituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆ alkyl)amino group, aC₁₋₆ alkyl group substituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆alkoxy)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₆alkylsulfonyl)-N-(C₁₋₆ alkyl)amino group, a C₁₋₆ alkyl group substitutedby an N-(C₁₋₆ alkylsulfonyl)-N-(C₁₋₆ alkoxy)amino group, a phenyl group(provided that such a phenyl group may be substituted by one or moresubstituents selected from the group consisting of a halogen atom, atrifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxygroup and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substitutedby a phenyl group (provided that such a phenyl group may be substitutedby one or more substituents selected from the group consisting of ahalogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkylgroup, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₂₋₇alkenyl group substituted by a phenyl group (provided that such a phenylgroup may be substituted by one or more substituents selected from thegroup consisting of a halogen atom, a trifluoromethyl group, a nitrogroup, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonylgroup), a C₂₋₆ alkynyl group substituted by a phenyl group (providedthat such a phenyl group may be substituted by one or more substituentsselected from the group consisting of a halogen atom, a trifluoromethylgroup, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenoxy group(provided that such a phenoxy group may be substituted by one or moresubstituents selected from the group consisting of a halogen atom, atrifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxygroup and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substitutedby a phenylthio group (provided that such a phenylthio group may besubstituted by one or more substituents selected from the groupconsisting of a halogen atom, a trifluoromethyl group, a nitro group, aC₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),a C₁₋₆ alkyl group substituted by a phenylsulfinyl group (provided thatsuch a phenylsulfinyl group may be substituted by one or moresubstituents selected from the group consisting of a halogen atom, atrifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxygroup and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substitutedby a phenylsulfonyl group (provided that such a phenylsulfonyl group maybe substituted by one or more substituents selected from the groupconsisting of a halogen atom, a trifluoromethyl group, a nitro group, aC₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),a C₁₋₆ alkyl group substituted by a benzyloxy group (provided that thephenyl group of such a benzyloxy group may be substituted by one or moresubstituents selected from the group consisting of a halogen atom, atrifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxygroup and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substitutedby a benzylthio group (provided that the phenyl group of such abenzylthio group may be substituted by one or more substituents selectedfrom the group consisting of a halogen atom, a trifluoromethyl group, anitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by abenzylsulfinyl group (provided that the phenyl group of such abenzylsulfinyl group may be substituted by one or more substituentsselected from the group consisting of a halogen atom, a trifluoromethylgroup, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by abenzylsulfonyl group (provided that the phenyl group of such abenzylsulfonyl group may be substituted by one or more substituentsselected from the group consisting of a halogen atom, a trifluoromethylgroup, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by aphenylcarbonyl group (provided that such a phenylcarbonyl group may besubstituted by one or more substituents selected from the groupconsisting of a halogen atom, a trifluoromethyl group, a nitro group, aC₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),a C₁₋₆ alkyl group substituted by a benzylcarbonyl group (provided thatthe phenyl group of such a benzylcarbonyl group may be substituted byone or more substituents selected from the group consisting of a halogenatom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl groupsubstituted by an amino group substituted by a C₁₋₄ alkylsulfonyl group,or a C₁₋₆ alkyl group substituted by an amino group substituted by aC₂₋₄ alkylcarbonyl group,

R^(f2) is a C₁₋₈ alkyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynylgroup, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylthio group, a C₁₋₆alkyl group substituted by a C₁₋₆ alkylsulfinyl group, a C₁₋₆ alkylgroup substituted by a C₁₋₆ alkylsulfonyl group, a C₁₋₆ alkyl groupsubstituted by a C₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by aC₂₋₇ alkoxycarbonyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a cyano group, aphenyl group (provided that such a phenyl group may be substituted byone or more substituents selected from the group consisting of a halogenatom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆alkoxy group and a C₂₋₇ alkoxycarbonyl group), or a C₁₋₆ alkyl groupsubstituted by a phenyl group (provided that such a phenyl group may besubstituted by one or more substituents selected from the groupconsisting of a halogen atom, a trifluoromethyl group, a nitro group, aC₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),

each of R^(f3), R^(f4), R^(f7), R^(f8), R^(f11) and R^(f12) which areindependent of one another, is a hydrogen atom, a C₁₋₆ alkyl group, amono-, di- or poly-halogeno C₁₋₆ alkyl group, a C₁₋₆ alkoxy group, amono-, di- or poly-halogeno C₁₋₆ alkoxy group, a C₁₋₆ alkylthio group, aC₁₋₆ alkylsulfinyl group, a C₁₋₆ alkylsulfonyl group, a C₂₋₇alkoxycarbonyl group, a C₂₋₇ alkylcarbonyl group, a halogen atom, anitro group, a cyano group, or a phenyl group (provided that such aphenyl group may be substituted by one or more substituents selectedfrom the group consisting of a halogen atom, a trifluoromethyl group, anitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group),

each of R^(f5), R^(f6), R^(f9), R^(f10), R^(f13), R^(f14) and R^(f15)which are independent of one another, is a hydrogen atom, a C₁₋₈ alkylgroup, a C₂₋₈ alkenyl group, a C₂₋₈ alkynyl group, or a phenyl group(provided that such a phenyl group may be substituted by one or moresubstituents selected from the group consisting of a halogen atom, atrifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxygroup and a C₂₋₇ alkoxycarbonyl group),

R^(g1) is a C₁₋₈ alkyl group, a C₃₋₇ cycloalkyl group, a C₁₋₆ alkylgroup substituted by a C₃₋₇ cycloalkyl group, a C₃₋₇ cycloalkenyl group,a C₁₋₆ alkyl group substituted by a C₃₋₇ cycloalkenyl group, a C₂₋₈alkenyl group, a C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by aC₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkenyloxygroup, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkynyloxy group, a C₁₋₆alkyl group substituted by a mono-, di- or poly-halogeno C₁₋₆ alkoxygroup, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogenoC₂₋₆ alkenyloxy group, a C₁₋₆ alkyl group substituted by a mono-, di- orpoly-halogeno C₂₋₆ alkynyloxy group, a C₁₋₆ alkyl group substituted by aC₁₋₆ alkylthio group, a C₁₋₆ alkyl group substituted by a C₁₋₆alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆alkylsulfonyl group, a mono-, di- or poly-halogeno C₁₋₈ alkyl group, amono-, di- or poly-halogeno C₂₋₈ alkenyl group, a mono-, di- orpoly-halogeno C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by acyano group, a C₂₋₆ alkenyl group substituted by a cyano group, a C₂₋₆alkynyl group substituted by a cyano group, a C₁₋₆ alkyl groupsubstituted by a nitro group, a C₂₋₆ alkenyl group substituted by anitro group, a C₂₋₆ alkynyl group substituted by a nitro group, a C₁₋₆alkyl group substituted by a C.sub. 2-7 alkoxycarbonyl group, a C₂₋₆alkenyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkynylgroup substituted by a C₂₋₇ alkoxycarbonyl group, a C₁₋₆ alkyl groupsubstituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl groupsubstituted by a mono-, di- or poly-halogeno C₂₋₇ alkylcarbonyl group, aC₁₋₆ alkyl group substituted by a C₃₋₇ alkenylcarbonyl group, a C₁₋₆alkyl group substituted by a C₃₋₇ alkynylcarbonyl group, a C₁₋₆ alkylgroup substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonylgroup substituted by a C₁₋₄ alkylthio group, a C₁₋₆ alkyl groupsubstituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₂₋₅alkylcarbonyl group substituted by a C₁₋₄ alkylsulfonyl group, a C₂₋₆alkenyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₂₋₆ alkynylgroup substituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl groupsubstituted by a C₁₋₆ alkylsulfamoyl group, a C₁₋₆ alkyl groupsubstituted by a C₁₋₆ alkoxysulfamoyl group, a C₁₋₆ alkyl groupsubstituted by a di(C₁₋₃ alkyl)sulfamoyl group, a C₁₋₆ alkyl groupsubstituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)sulfamoyl group, a C₁₋₆alkyl group substituted by a C₂₋₇ alkylcarbamoyl group, a C₁₋₆ alkylgroup substituted by a di(C₁₋₃ alkyl)carbamoyl group, a C₁₋₆ alkyl groupsubstituted by a C₂₋₇ alkoxycarbamoyl group, a C₁₋₆ alkyl groupsubstituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)carbamoyl group, a C₁₋₆alkyl group substituted by a C₁₋₆ alkylamino group, a C₁₋₆ alkyl groupsubstituted by a C₁₋₆ alkoxyamino group, a C₁₋₆ alkyl group substitutedby a di(C₁₋₃ alkyl)amino group, a C₁₋₆ alkyl group substituted by anN-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)amino group, a C₁₋₆ alkyl groupsubstituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆ alkyl)amino group, aC₁₋₆ alkyl group substituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆alkoxy)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₆alkylsulfonyl)-N-(C₁₋₆ alkyl)amino group, a C₁₋₆ alkyl group substitutedby an N-(C₁₋₆ alkylsulfonyl)-N-(C₁₋₆ alkoxy)amino group, a C₁₋₆ alkylgroup substituted by a phenyl group (provided that such a phenyl groupmay be substituted by one or more substituents selected from the groupconsisting of a halogen atom, a trifluoromethyl group, a nitro group, aC₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),a C₂₋₇ alkenyl group substituted by a phenyl group (provided that such aphenyl group may be substituted by one or more substituents selectedfrom the group consisting of a halogen atom, a trifluoromethyl group, anitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₂₋₆ alkynyl group substituted by a phenylgroup (provided that such a phenyl group may be substituted by one ormore substituents selected from the group consisting of a halogen atom,a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl groupsubstituted by a phenoxy group (provided that such a phenoxy group maybe substituted by one or more substituents selected from the groupconsisting of a halogen atom, a trifluoromethyl group, a nitro group, aC₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),a C₁₋₆ alkyl group substituted by a phenylthio group (provided that sucha phenylthio group may be substituted by one or more substituentsselected from the group consisting of a halogen atom, a trifluoromethylgroup, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by aphenylsulfinyl group (provided that such a phenylsulfinyl group may besubstituted by one or more substituents selected from the groupconsisting of a halogen atom, a trifluoromethyl group, a nitro group, aC₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),a C₁₋₆ alkyl group substituted by a phenylsulfonyl group (provided thatsuch a phenylsulfonyl group may be substituted by one or moresubstituents selected from the group consisting of a halogen atom, atrifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxygroup and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substitutedby a benzyloxy group (provided that the phenyl group of such a benzyloxygroup may be substituted by one or more substituents selected from thegroup consisting of a halogen atom, a trifluoromethyl group, a nitrogroup, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonylgroup), a C₁₋₆ alkyl group substituted by a benzylthio group (providedthat the phenyl group of such a benzylthio group may be substituted byone or more substituents selected from the group consisting of a halogenatom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl groupsubstituted by a benzylsulfinyl group (provided that the phenyl group ofsuch a benzylsulfinyl group may be substituted by one or moresubstituents selected from the group consisting of a halogen atom, atrifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxygroup and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substitutedby a benzylsulfonyl group (provided that the phenyl group of such abenzylsulfonyl group may be substituted by one or more substituentsselected from the group consisting of a halogen atom, a trifluoromethylgroup, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by aphenylcarbonyl group (provided that such a phenylcarbonyl group may besubstituted by one or more substituents selected from the groupconsisting of a halogen atom, a trifluoromethyl group, a nitro group, aC₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),or a C₁₋₆ alkyl group substituted by a benzylcarbonyl group (providedthat the phenyl group of such a benzylcarbonyl group may be substitutedby one or more substituents selected from the group consisting of ahalogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkylgroup, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),

each of R^(g2) and R^(g3) which are independent of each other, is a C₁₋₆alkyl group, a C₂₋₆ alkenyl group, a C₂₋₆ alkynyl group, a mono-, di- orpoly-halogeno C₁₋₆ alkyl group, a C₁₋₆ alkoxy group, a C₁₋₆alkylsulfonyl group, a C₁₋₆ alkylsulfamoyl group, a di(C₁₋₃alkyl)sulfamoyl group, a C₂₋₇ alkoxycarbonyl group, a C₂₋₇ alkylcarbonylgroup, a C₂₋₇ alkylcarbamoyl group, a di(C₁₋₃ alkyl)carbamoyl group, aphenyl group (provided that such a phenyl group may be substituted byone or more substituents selected from the group consisting of a halogenatom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆alkoxy group and a C₂₋₇ alkoxycarbonyl group), or a benzyl group(provided that the phenyl group of such a benzyl group may besubstituted by one or more substituents selected from the groupconsisting of a halogen atom, a trifluoromethyl group, a nitro group, aC₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),

or R^(g2) and R^(g3) form a saturated 3- to 7-membered heterocyclic ringtogether with the nitrogen atom to which they are bonded,

X is an oxygen atom or a sulfur atom,

L is a hydrogen atom, a C₁₋₆ alkyl group, a C₂₋₆ alkenyl group or a C₂₋₆alkynyl group,

G is ##STR3##

A is a CH group, or a nitrogen atom, and

each of B and D which are independent of each other, is a C₁₋₄ alkylgroup, a C₁₋₄ alkoxy group, a mono-, di- or poly-halogeno C₁₋₄ alkylgroup, a mono-, di- or poly-halogeno C₁₋₄ alkoxy group, a halogen atom,a C₁₋₄ alkylamino group, or a di(C₁₋₄ alkyl)amino group, (hereinafterreferred to as the compound of the present invention) exhibitsremarkably strong herbicidal activities against many weeds in soiltreatment, in soil admixing treatment or in foliage treatment and at thesame time has a high level of safety for important crop plants such aswheat, corn, cotton, soybean, sugar beet and rice, etc. The presentinvention has been accomplished on the basis of this discovery.

Examples for the substituents R^(a1), R^(a2), R^(a3), R^(a4), R^(a5),R^(a6), R^(b1), R^(b2), R^(b3), R^(b4), R^(b5), R^(c1), R^(c2), R^(c3),R^(c4), R^(c5), R^(c6), R^(c7), R^(c8), R^(c9), R^(c10), R^(c11),R^(c12), R^(c13), R^(c14), R^(d1), R^(d2), R^(d3), R^(d4), R^(d5),R^(d6), R^(e1), R^(e2), R^(e3), R^(e4), R^(e5), R^(e6), R^(e7), R^(e8),R^(e9), R^(e10), R^(f1), R^(f2), R^(f3), R^(f4), R^(f5), R^(f6), R^(f7),R^(f8), R^(f9), R^(f10), R^(f11), R^(f12), R^(f13), R^(f14), R^(f15),R^(g1), R^(g2), R^(g3) L, B and D of the compound of the presentinvention are as follows. However, symbols have the following meanings.

Me: methyl group, Et: ethyl group, Pr-n: n-propyl group, Pr-iso:isopropyl group, Bu-n: n-butyl group, Bu-iso: isobutyl group, Bu-sec:sec-butyl group, Bu-tert: tert-butyl group, Pen-n: n-pentyl group,Hex-n: n-hexyl group, Hep-n: n-heptyl group, Pr-cyc: cyclopropyl group,Bu-cyc: cyclobutyl group, Pen-cyc: cyclopentyl group, Hex-cyc:cyclohexyl group, and Ph: phenyl group.

Specific examples for the substituents R^(a1), R^(b1), R^(d1), R^(e1)and R^(f1) of the compound of the present invention

Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, Pen-n, Hex-n,Hep-n, Pr-cyc, Bu-cyc, Pen-cyc, Hex-cyc, CH₂ Pr-cyc, CH₂ CH₂ Pr-cyc,CHMe-Pr-cyc, CH₂ CHMe-Pr-cyc, CHMeCH₂ Pr-cyc, CH₂ Bu-cyc, CH₂ CH₂Bu-cyc, CH₂ Pen-cyc, CH₂ Hex-cyc, ##STR4## CH₂ CH═CH₂, CH₂ CH═CHMe, CH₂CH═CHEt, CH₂ CH₂ CH═CH₂, CH₂ CH₂ CH═CHMe, CH₂ CH═CMe₂, CHMeCH═CH₂, CH₂CMe═CH₂, CH₂ CMe═CHMe, CHMeCH═CHMe, CH₂ CMe═CHEt, CH₂ CH₂ CH═CMe₂, CH₂CMe═CMe₂, CH₂ C.tbd.CH, CH₂ C.tbd.CMe, CH₂ C.tbd.CEt, CH₂ CH₂ C.tbd.CH,CH₂ CH₂ C.tbd.CMe, CHMeC.tbd.CH, CHMeC.tbd.CMe, CH₂ OMe, CH₂ OEt, CH₂OPr-n, CH₂ OPr-iso, CH₂ CH₂ OMe, CH₂ CH₂ OEt, CH₂ CH₂ OPr-n, CHMeOMe,CHMeOEt, CH₂ CHMeOMe, CH₂ CHMeOEt, CH₂ CH₂ CH₂ OMe, CH₂ CH₂ CH₂ OEt, CH₂OCH₂ CH═CH₂, CH₂ OCH₂ CH═CHMe, CH₂ CH₂ OCH₂ CH═CH₂, CH₂ CH₂ OCH₂CH═CHMe, CH₂ OCH₂ C.tbd.CH, CH₂ OCH₂ C.tbd.CMe, CH₂ OCHMeC.tbd.CH, CH₂OCMe₂ C.tbd. CH, CH₂ CH₂ OCH₂ C.tbd.CH, CH₂ CH₂ OCH₂ C.tbd.CMe, CH₂ CH₂OCHMeC.tbd.CH, CH₂ CH₂ OCMe₂ C.tbd.CH, CH₂ OCHF₂, CH₂ OCF₃, CH₂ OCF₂CF₃, CH₂ CH₂ OCHF₂, CH₂ CH₂ OCF₃, CH₂ CH₂ OCF₂ CF₃, CH₂ OCH₂ CF₃, CH₂CH₂ OCH₂ CF₃, CH₂ OCH₂ CHF₂, CH₂ CH₂ OCH₂ CHF₂, CH₂ OCH₂ CH₂ F, CH₂ OCH₂CH₂ Cl, CH₂ OCH₂ CH₂ Br, CH₂ CH₂ OCH₂ CH₂ F, CH₂ CH₂ OCH₂ CH₂ Cl, CH₂CH₂ OCH₂ CH₂ Br, CH₂ OCH₂ CH═CHCl, CH₂ CH₂ OCH₂ CH═CHCl, CH₂ OCH₂CH═CHBr, CH₂ CH₂ OCH₂ CH═CHBr, CH₂ OCH₂ CF═CF₂, CH₂ CH₂ OCH₂ CF═CF₂, CH₂OCH═ CHCl, CH₂ CH₂ OCH═CHCl, CH₂ OCF═CF₂, CH₂ CH₂ OCF═CF₂, CH₂ OCF₂CF═CF₂, CH₂ CH₂ OCF₂ CF═CF₂, CH₂ OCH₂ CH═CF₂, CH₂ CH₂ OCH₂ CH═CF₂, CH₂OCH₂ CH═CHCF₃, CH₂ CH₂ OCH₂ CH═CHCF₃, CH₂ OCH₂ C.tbd.CI, CH₂ OCH₂ CH₂C.tbd.CI, CH₂ CH₂ OCH₂ C.tbd.CI, CH₂ OCH₂ C.tbd.CCF₃, CH₂ CH₂ OCH₂C.tbd.CCF₃, CH₂ OCMe₂ C.tbd.CI, CH₂ CH₂ OCMe₂ C.tbd.CI, CH₂ OCMe₂C.tbd.CCF₃, CH₂ CH₂ OCMe₂ C.tbd.CCF₃, CH₂ SMe, CH₂ SEt, CH₂ SPr-n, CH₂CH₂ SMe, CH₂ CH₂ SEt, CH₂ CH₂ SPr-n, CHMeSMe, CHMeSEt, CH₂ CHMeSMe, CH₂CHMeSEt, CH₂ SOMe, CH₂ SOEt, CH₂ SOPr-n, CH₂ CH₂ SOMe, CH₂ CH₂ SOEt,CH.sub. 2 CH₂ SOPr-n, CHMeSOMe, CHMeSOEt, CH₂ CHMeSOMe, CH₂ CHMeSOEt,CH₂ SO₂ Me, CH₂ SO₂ Et, CH₂ SO₂ Pr-n, CH₂ CH₂ SO₂ Me, CH₂ CH₂ SO₂ Et,CH₂ CH₂ SO₂ Pr-n, CHMeSO₂ Me, CHMeSO₂ Et, CH₂ CHMeSO₂ Me, CH₂ CHMeSO₂Et, CH₂ CH₂ F, CH₂ CHF₂, CH₂ CF₃, CH₂ CH₂ Cl, CH₂ CH₂ Br, CH₂ CCl₃, CH₂CH₂ CF₃, CH₂ CH₂ CCl₃, CH₂ CH₂ CH₂ F, CH₂ CH₂ CH₂ Cl, CF₂ CF₃, CH₂ CF₂CF₃, CH₂ CH═CHCl, CH₂ CH═CHBr, CH₂ CH═CF₂, CH₂ CF═CF₂, CH₂ CH═CHCF₃, CH₂CH═CBrMe, CH₂ CH═CClMe, CH₂ CH═C(CF₃)Me, CF₂ CF═CF₂, CH₂ C.tbd.CI, CH₂CH₂ C.tbd.CI, CH₂ C.tbd.CCF₃, CH₂ CH₂ C.tbd.CCF₃, CH₂ CN, CH₂ CH₂ CN,CHMeCN, CH₂ CHMeCN, CH₂ CMe₂ CN, CH₂ CH═CHCN, CH₂ CH(CN)CH═CH₂, CH₂C(CN)═CH₂, CH₂ C(CN)═CHMe, CH₂ CH(CN)C.tbd.CH, CH₂ CH(CN)C.tbd.C-Me,CH(CN)C.tbd.CH, CH₂ NO₂, CH₂ CH₂ NO₂, CH₂ CHMeNO₂, CH₂ CMe₂ NO₂, CH₂ CH₂CH₂ NO₂, CH₂ CH.tbd.CHNO₂, CH₂ CH(NO₂)CH═CH₂, CH₂ C(NO₂)═CH₂, CH₂C(NO₂)═CHMe, CH₂ CH(NO₂)C.tbd.CH, CH₂ CH(NO₂)C.tbd.CMe, CH₂ CO₂ Me, CH₂CO₂ Et, CH₂ CO₂ Pr-n, CH₂ CO₂ Pr-iso, CH₂ CO₂ Bu-n, CHMeCO₂ Me, CHMeCO₂Et, CH₂ CH₂ CO₂ Me, CH₂ CH₂ CO₂ Et, CH₂ CHMeCO₂ Me, CH₂ CH₂ CH₂ CO₂ Me,CH₂ CH═CHCO₂ Me, CH₂ CH═CHCO₂ Et, CH₂ CH═CHCO₂ Pr-n, CH₂ CH═CMeCO₂ Me,CH₂ CMe═CHCO₂ Me, CHMeCH═CHCO₂ Me, CHMeCH═CHCO₂ Et, CH₂ CH₂ CH═CHCO₂ Me,CH.sub. 2 CH═CHCH₂ CO₂ Me, CH₂ C.tbd.CCO₂ Me, CH₂ C.tbd.CCO₂ Et, CH₂C.tbd.CCO₂ Pr-n, CH₂ CH₂ C.tbd.CCO₂ Me, CH₂ CHMeC.tbd.CCO₂ Me, CH₂ CMe₂C.tbd.CCO₂ Me, CH₂ C.tbd.CCH₂ CO₂ Me, CH₂ COMe, CH₂ COEt, CH₂ COPr-n,CH₂ CH₂ COMe, CH₂ CH₂ COEt, CH₂ CHMeCOMe, CH₂ CMe₂ COMe, CH₂ COCF₃, CH₂COCCl₃, CH₂ CH₂ COCF₃, CH₂ COCH₂ CF₃, CH₂ COCH₂ CHF₂, CH₂ COCH₂ CHCl₂,CH₂ COCH₂ F, CH₂ COCH₂ Cl, CH₂ COCH₂ Br, CH₂ COCH═CH₂, CH₂ COCH═CHMe,CH₂ COCH₂ CH═CH₂, CH₂ CH₂ COCH═CH₂, CH₂ CH₂ COCH═CHMe, CH₂ COC.tbd.CH,CH₂ COC.tbd.CMe, CH₂ COCH₂ C.tbd.CH, CH₂ CH₂ COC.tbd.CH, CH₂ CH₂COC.tbd.CMe, CH₂ COCH₂ OMe, CH₂ COCH₂ OEt, CH₂ COCH₂ CH₂ OMe, CH₂ COCH₂CH₂ OEt, CH₂ CH₂ COCH₂ OMe, CH₂ CH₂ COCH₂ OEt, CH₂ COCH₂ SMe, CH₂ COCH₂SEt, CH₂ COCH₂ CH₂ SMe, CH₂ COCH₂ CH₂ SEt, CH₂ CH₂ COCH₂ SMe, CH₂ CH₂COCH₂ SEt, CH₂ COCH₂ SOMe, CH₂ COCH₂ SOEt, CH₂ COCH₂ CH₂ SOMe, CH₂ COCH₂CH₂ SOEt, CH₂ CH₂ COCH₂ SOMe, CH₂ CH₂ COCH₂ SOEt, CH₂ COCH₂ SO₂ Me, CH₂COCH₂ SO₂ Et, CH₂ COCH₂ CH₂ SO₂ Me, CH₂ COCH₂ CH₂ SO₂ Et, CH₂ CH₂ COCH₂SO₂ Me, CH₂ CH₂ COCH₂ SO₂ Et, CH₂ CH═CHCOMe, CH₂ CH═CHCOEt,CHMeCH═CHCOMe, CHMeCH═CHCOEt, CH₂ C═CCOMe, CH₂ C.tbd.CCOEt,CHMeC.tbd.CCOMe, CHMeC.tbd.CCOEt, CH₂ SO₂ NHMe, CH₂ SO₂ NHEt, CH₂ SO₂NHPr-n, CH.sub. 2 CH₂ SO₂ NHMe, CH₂ CH₂ SO₂ NHEt, CH₂ CH₂ SO₂ NHPr-n,CH₂ SO₂ NHOMe, CH₂ SO₂ NHOEt, CH₂ SO₂ NHOPr-n, CH₂ CH₂ SO₂ NHOMe, CH₂CH₂ SO₂ NHOEt, CH₂ CH₂ SO₂ NHOPr-n, CH₂ SO₂ NMe₂, CH₂ SO₂ NMeEt, CH₂ SO₂NEt₂, CH₂ CH₂ SO₂ NMe₂, CH₂ CH₂ SO₂ NMeEt, CH₂ CH₂ SO₂ NEt₂, CH₂ SO₂N(OMe)Me, CH₂ SO₂ N(OMe)Et, CH₂ SO₂ N(OEt)Me, CH₂ CH₂ SO₂ N(OMe)Me, CH₂CH₂ SO₂ N(OMe)Et, CH₂ CH₂ SO₂ N(OEt)Me, CH₂ SO₂ N(OEt)Et, CH₂ CH₂ SO₂N(OEt)Et, CH₂ CONHMe, CH₂ CONHEt, CH₂ CONHPr-n, CH₂ CH₂ CONHMe, CH₂ CH₂CONHEt, CH₂ CH₂ CONHPr-n, CH₂ CONMe₂, CH₂ CONMeEt, CH₂ CONEt₂, CH₂ CH₂CONMe₂, CH₂ CH₂ CONMeEt, CH₂ CH₂ CONEt₂, CH₂ CONHOMe, CH₂ CONHOEt, CH₂CONHOPr-n, CH₂ CH₂ CONHOMe, CH₂ CH₂ CONHOEt, CH₂ CH₂ CONHOPr-n, CH₂CON(OMe)Me, CH₂ CON(OMe)Et, CH₂ CON(OEt)Me, CH₂ CH₂ CON(OMe)Me, CH₂ CH₂CON(OMe)Et, CH₂ CH₂ CON(OEt)Me, CH₂ CON(OEt)Et, CH₂ CH₂ CON(OEt)Et, CH₂NHMe, CH₂ NHEt, CH₂ NHPr-n, CH₂ CH₂ NHMe, CH₂ CH₂ NHEt, CH₂ CH₂ NHPr-n,CH₂ CHMeNHMe, CH₂ CHMeNHEt, CH₂ CHMeNHPr-n, CH₂ CH₂ CH₂ NHMe, CH₂ NHOMe,CH₂ NHOEt, CH₂ NHOPr-n, CH₂ CH₂ NHOMe, CH₂ CH₂ NHOEt, CH₂ CH₂ NHOPr-n,CH₂ CHMeNHOMe, CH₂ CHMeNHOEt, CH₂ CHMeNHOPr-n, CH₂ NMe₂, CH₂ NMeEt, CH₂NMePr-n, CH₂ CH₂ NMe₂, CH₂ CH₂ NMeEt, CH₂ CH₂ NMePr-n, CH₂ NEt₂ , CH₂CH₂ NEt₂, CH₂ N(OMe)Me, CH₂ N(OMe)Et, CH₂ N(OEt)Me, CH₂ N(OEt)Et, CH₂CH₂ N(OMe)Me, CH₂ CH₂ N(OMe)Et, CH₂ CH₂ N(OEt)Me, CH₂ CH₂ N(OEt)Et, CH₂NMeCOMe, CH₂ NEtCOMe, CH₂ NMeCOEt, CH₂ CH₂ NMeCOMe, CH₂ CH₂ NEtCOMe, CH₂CH₂ NMeCOEt, CH₂ N(OMe)COMe, CH₂ N(OEt)COMe, CH₂ N(OMe)COEt, CH₂ CH₂N(OMe)COMe, CH₂ CH₂ N(OEt)COMe, CH₂ CH₂ N(OMe)COEt, CH₂ NMeSO₂ Me, CH₂NEtSO₂ Me, CH₂ NMeSO₂ Et, CH₂ CH₂ NMeSO₂ Me, CH₂ CH₂ NEtSO₂ Me, CH₂ CH₂NMeSO₂ Et, CH₂ N(OMe)SO₂ Me, CH₂ N(OEt)SO₂ Me, CH₂ N(OMe)SO₂ Et, CH₂ CH₂N(OMe)SO₂ Me, CH₂ CH₂ N(OEt)SO₂ Me, CH₂ CH₂ N(OMe)SO₂ Et, CH₂ Ph, CH₂CH₂ Ph, CH₂ CH₂ CH₂ Ph, CHMePh, CH₂ CHMePh, CH₂ CMe₂ Ph, CH₂ CH═CHPh,CH₂ CH═CMePh, CHMeCH═CHPh, CH₂ CMe═CMePh, CHMeCMe═CMePh, CH₂ C.tbd.CPh,CHMeC.tbd.CPh, CH₂ CMe₂ C.tbd.CPh, CH₂ CH₂ OPh, CH₂ CHMeOPh, CH₂ CMe₂OPh, CH₂ OPh, CH₂ CH₂ SPh, CH₂ CHMeSPh, CH₂ CMe₂ SPh, CH₂ SPh, CH₂ CH₂SOPh, CH₂ CHMeSOPh, CH₂ CMe₂ SOPh, CH₂ CH₂ SO₂ Ph, CH₂ CHMeSO₂ Ph, CH₂CMe₂ SO₂ Ph, CH₂ OCH₂ Ph, CH₂ CH₂ OCH₂ Ph, CH₂ CHMeOCH₂ Ph, CH₂ SCH₂ Ph,CH₂ CH₂ SCH₂ Ph, CH₂ CHMeSCH₂ Ph, CH₂ SOCH₂ Ph, CH₂ CH₂ SOCH₂ Ph, CH₂CHMeSOCH₂ Ph, CH₂ SO₂ CH₂ Ph, CH₂ CH₂ SO₂ CH₂ Ph, CH₂ CHMeSO₂ CH₂ Ph,CH₂ COPh, CH₂ CH₂ COPh, CHMeCOPh, CH₂ COCH₂ Ph, CH₂ CH₂ COCH₂ Ph,CHMeCOCH₂ Ph, CH₂ C(Cl)═CH₂, Ph, CH₂ SOPh, CH₂ SO₂ Ph, CH₂ Ph-4-OMe, CH₂Ph-4-Cl, CH₂ C(Br)═CH₂, CH₂ C(Cl)═CHCl, CH₂ CH═C(I)Me, CH₂ CH═CHI, CH₂C(F)═CHCl, CH₂ CH═CBr₂, CH₂ CH═CHF, CH₂ C(Cl)═CHMe, CH₂ C(F)═CHBr, CH₂C(Br)═CHCl, CH₂ C(Br)═CCl₂, CH₂ CH═CHCH₂ F, CH₂ C(I)═CH₂, CH₂C(Br)═C(Cl)Me, CH₂ C(I)═CHMe, CH₂ C(Cl)═CCl₂, CH₂ CH═CHCCl₃, CH₂C(Br)═CHMe, CH₂ C(Cl)═CHF, CH₂ C(Br)═CHF, CH₂ CH═C(Cl)Br, CH₂C(F)═C(Cl)CF₃, CH₂ C(Cl)═C(Cl)Me, CH₂ C(Br)═CHBr, CH₂ CH═C(F)CF₂ Cl, CH₂C(Br)═C(Br)Me, CH₂ CH═C(F)CF₃, CH₂ CH═CCl₂, CH₂ C(F)═CH₂, CH₂ CH═CHCCl₃,CH₂ CH═C(F)Cl, CH₂ C(Cl)═C(F)Cl, CH₂ C(F)═CCl₂, CH₂ C(Cl)═CF₂, CH₂C(CF₃)═CH₂, CMe₂ CH═CH₂, CMe₂ C.tbd.CH, CH₂ CH₂ I, CH₂ C.tbd.C-CN, CH₂NHBu-n, CH₂ NHSO₂ Me, CH₂ NHSO₂ Et, CH₂ CH₂ NHSO₂ Me, CH₂ CH₂ NHSO₂ Et,CH₂ NHCOMe, CH₂ NHCOEt, CH₂ CH₂ NHCOMe, CH₂ CH₂ NHCOEt Specific examplesfor the substituents R^(a2) and R^(a3) of the compound of the presentinvention

H, Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, CH₂ F, CHF₂,CF₃, CH₂ Cl, CH₂ Br, CH₂ CF₃, CH₂ CH₂ F, CH₂ CH₂ Cl, CH₂ CH₂ Br, CF₂CF₃, OMe, OEt, OPr-n, OPr-iso, OCF₃, OCH₂ CF₃, SMe, SEt, SPr-n, SPr-iso,SOMe, SOEt, SOPr-n, SOPr-iso, SO₂ Me, SO₂ Et, SO₂ Pr-n, SO₂ Pr-iso, CO₂Me, CO₂ Et, CO₂ Pr-n, CO₂ Pr-iso, CO₂ Bu-n, COMe, COEt, COPr-n,COPr-iso, COBu-n, F, Cl, Br, I, NO₂, CN, Ph

Specific examples for the substituents R^(a4) and R^(a5) of the compoundof the present invention

H, Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, Pen-n, Hex-n,Hep-n, CH═CH₂, CH═CHMe, CH═CHEt, CMe═CH₂, CH═CMe₂, CMe═CHMe, CMe═CMe₂,CH₂ CH═CH₂, CH₂ CH₂ CHMe, CHMeCH═CH₂, CHMeCH═CHMe, CMe₂ CH═CH₂, CMe₂CH═CHMe, C.tbd.CH, C.tbd.CMe, C.tbd.CEt, CH₂ C.tbd.CH, CH₂ C.tbd.CMe,CHMeC.tbd.CH, CHMeC.tbd.CMe, CMe₂ C.tbd.CH, CMe₂ C.tbd.CMe, Ph

Specific examples for the substituent R^(a6) of the compound of thepresent invention

Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, Pen-n, Hex-n,Hep-n, CH₂ CH═CH₂, CH₂ CH═CHMe, CH₂ CH═CHEt, CH₂ CH₂ CH═CH₂, CH₂ CH₂CH═CHMe, CH₂ CH═CMe₂, CHMeCH═CH₂, CH₂ CMe═CH₂, CH₂ CMe═CHMe,CHMeCH═CHMe, CH₂ CMe═CHEt, CH₂ CH₂ CH═CMe₂, CH₂ CMe═CMe₂, CMe₂ CH═CH₂,CMe₂ CH═CHMe, CH₂ C.tbd.CH, CH₂ C.tbd.CMe, CH₂ C.tbd.CEt, CH₂ CH₂C.tbd.CH, CH₂ CH₂ C.tbd.CMe, CHMeC.tbd.CH, CHMeC.tbd.CMe, CMe₂ C.tbd.CH,CMe₂ C.tbd.CMe, Ph

Specific examples for the substituent R^(b2) of the compound of thepresent invention

H, Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, CH₂ F, CHF₂,CF₃, CH₂ Cl, CH₂ Br, CH₂ CF₃, CH₂ CH₂ F, CH₂ CH₂ Cl, CH₂ CH₂ Br, CF₂CF₃, OMe, OEt, OPr-n, OPr-iso, OCF₃, OCH₂ CF₃, SMe, SEt, SPr-n, SPr-iso,SOMe, SOEt, SOPr-n, SOPr-iso, SO₂ Me, SO₂ Et, SO₂ Pr-n, SO₂ Pr-iso, CO₂Me, CO₂ Et, CO₂ Pr-n, CO₂ Pr-iso, CO₂ Bu-n, COMe, COEt, COPr-n,COPr-iso, COBu-n, F, Cl, Br, I, NO₂, CN, Ph

Specific examples for the substituent R^(b3) of the compound of thepresent invention

Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, Pen-n, Hex-n, CH₂CH═CH₂, CH₂ CH═CHMe, CH₂ CH═CHEt, CH₂ CH₂ CH═CH₂, CH₂ CH₂ CH═CHMe, CH₂CH═CMe₂, CHMeCH═CH₂, CH₂ CMe═CH₂, CH₂ CMe═CHMe, CHMeCH═CHMe, CH₂CMe═CHEt, CH₂ CH₂ CH═CMe₂, CH₂ CMe═CME₂, CH₂ C.tbd.CH, CH₂ C.tbd.CMe,CH₂ C.tbd.CEt, CH₂ CH₂ C.tbd.CH, CH₂ CH₂ C.tbd.CMe, CHMeC.tbd.CH,CHMeC.tbd.CMe

Specific examples for the substituent R^(b4) of the compound of thepresent invention

H, Me, Et, Pr-n, Pr-iso, Bu-n, Pen-n, Hex-n

Specific examples for the substituent R^(b5) of the compound of thepresent invention

H, Me, Et, Pr-n, Pr-iso, Bu-n, Pen-n, Hex-n

Specific examples for the substituent R^(c1) of the compound of thepresent invention

Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, Pen-n, Hex-n,Hep-n, Pr-cyc, Bu-cyc, Pen-cyc, Hex-cyc, CH₂ Pr-cyc, CH₂ CH₂ Pr-cyc,CHMe-Pr-cyc, CH₂ CHMe-Pr-cyc, CHMeCH₂ Pr-cyc, CH₂ Bu-cyc, CH₂ CH₂Bu-cyc, CH₂ Pen-cyc, CH₂ Hex-cyc, ##STR5## CH₂ CH═CH₂, CH₂ CH═CHMe, CH₂CH═CHEt, CH₂ CH₂ CH═CH₂, CH₂ CH₂ CH═CHMe, CH₂ CH═CMe₂, CHMeCH═CH₂, CH₂CMe═CH₂, CH₂ CMe═CHMe, CHMeCH═CHMe, CH₂ CMe═CHEt, CH₂ CH₂ CH═CMe₂, CH₂CMe═CMe₂, CH₂ C.tbd.CH, CH₂ C.tbd.CMe, CH₂ C.tbd.CEt, CH₂ CH₂ C.tbd.CH,CH₂ CH₂ C.tbd.CMe, CHMeC.tbd.CH, CHMeC.tbd.CMe, CH₂ OMe, CH₂ OEt, CH₂OPr-n, CH₂ OPr-iso, CH₂ CH₂ OMe, CH₂ CH₂ OEt, CH₂ CH₂ OPr-n, CHMeOMe,CHMeOEt, CH₂ CHMeOMe, CH₂ CHMeOEt, CH₂ CH₂ CH₂ OMe, CH₂ CH₂ CH₂ OEt, CH₂OCH₂ CH═CH₂, CH₂ OCH₂ CH═CHMe, CH₂ CH₂ OCH₂ CH═CH₂, CH₂ CH₂ OCH₂CH═CHMe, CH₂ OCH₂ C.tbd.CH, CH₂ OCH₂ C.tbd.CMe, CH₂ OCHMeC.tbd.CH, CH₂OCMe₂ C.tbd.CH, CH₂ CH₂ OCH₂ C.tbd.CH, CH₂ CH₂ OCH₂ C.tbd.CMe, CH₂ CH₂OCHMeC.tbd.CH, CH₂ CH₂ OCMe₂ C.tbd.CH, CH₂ OCHF₂, CH₂ OCF₃, CH₂ OCF₂CF₃, CH₂ CH₂ OCHF₂, CH₂ CH₂ OCF₃, CH₂ CH₂ OCF₂ C₃, CH₂ OCH₂ CF₃, CH₂ CH₂OCH₂ CF₃, CH₂ OCH₂ CHF₂, CH₂ CH₂ OCH₂ CHF₂, CH₂ OCH₂ CH₂ F, CH₂ OCH₂ CH₂Cl, CH₂ OCH₂ CH₂ Br, CH₂ CH₂ OCH₂ CH₂ F, CH₂ CH₂ OCH₂ CH₂ Cl, CH₂ CH₂OCH₂ CH₂ Br, CH₂ OCH₂ CH═CHCl, CH₂ CH₂ OCH₂ CH═CHCl, CH₂ OCH₂ CH═CHBr,CH₂ CH₂ OCH₂ CH═CHBr, CH₂ OCH₂ CF═CF₂, CH₂ CH₂ OCH₂ CF═CF₂, CH₂OCH═CHCl, CH₂ CH₂ OCH═CHCl, CH₂ OCF═CF₂, CH₂ CH₂ OCF═CF₂, CH₂ OCF₂CF═CF₂, CH₂ CH₂ OCF₂ CF═CF₂, CH₂ OCH₂ CH═CF₂, CH₂ CH₂ OCH₂ CH═CF₂, CH₂OCH₂ CH═CHCF₃, CH₂ CH₂ OCH₂ CH═CHCF₃, CH₂ OCH₂ C.tbd.CI, CH₂ OCH₂ CH₂C.tbd.CI, CH₂ CH₂ OCH₂ C.tbd.CI, CH₂ OCH₂ C.tbd.CCF₃, CH₂ CH₂ OCH₂C.tbd.CCF₃, CH₂ OCMe₂ C.tbd.CI, CH₂ CH₂ OCMe₂ C.tbd.CI, CH₂ OCMe₂C.tbd.CCF₃, CH₂ CH₂ OCMe₂ C.tbd.CCF₃, CH₂ SMe, CH₂ SEt, CH₂ SPr-n, CH₂CH₂ SMe, CH₂ CH₂ SEt, CH₂ CH₂ SPr-n, CHMeSMe, CHMeSEt, CH₂ CHMeSMe, CH₂CHMeSEt, CH₂ SOMe, CH₂ SOEt, CH.sub. 2 SOPr-n, CH₂ CH₂ SOMe, CH₂ CH₂SOEt, CH₂ CH₂ SOPr-n, CHMeSOMe, CHMeSOEt, CH₂ CHMeSOMe, CH₂ CHMeSOEt,CH₂ SO₂ Me, CH₂ SO₂ Et, CH₂ SO₂ Pr-n, CH₂ CH₂ SO₂ Me, CH₂ CH₂ SO₂ Et,CH₂ CH₂ SO₂ Pr-n, CHMeSO₂ Me, CHMeSO₂ Et, CH₂ CHMeSO₂ Me, CH₂ CHMeSO₂Et, CH₂ CH₂ F, CH₂ CHF₂, CH₂ CF₃, CH₂ CH₂ Cl, CH₂ CH₂ Br, CH₂ CCl₃, CH₂CH₂ CF₃, CH₂ CH₂ CCl₃, CH₂ CH₂ CH₂ F, CH₂ CH₂ CH₂ Cl, CF₂ CF₃, CH₂ CF₂CF₃, CH₂ CH═CHCl, CH₂ CH═CHBr, CH₂ CH═CF₂, CH₂ CF═CF₂, CH₂ CH═CHCF₃, CH₂CH═CBrMe, CH₂ CH═CClMe, CH₂ CH═C(CF₃)Me, CF₂ CF═CF₂, CH₂ C.tbd.CI, CH₂CH.sub. 2 C.tbd.CI, CH₂ C.tbd.CCF₃, CH₂ CH₂ C.tbd.CCF₃, CH₂ CN, CH₂ CH₂CN, CHMeCN, CH₂ CHMeCN, CH₂ CMe₂ CN, CH₂ CH═CHCN, CH₂ CH(CN)CH═CH₂, CH₂C(CN)═CH₂, CH₂ C(CN)═CHMe, CH₂ CH(CN)C.tbd.CH, CH₂ CH(CN)C.tbd.C-Me,CH(CN)C.tbd.CH, CH₂ NO₂, CH₂ CH₂ NO₂, CH₂ CHMeNO₂, CH₂ CMe₂ NO₂, CH₂ CH₂CH₂ NO₂, CH₂ CH═CHNO₂, CH₂ CH(NO₂)CH═CH₂, CH₂ C(NO₂)═CH₂, CH₂C(NO₂)═CHMe, CH₂ CH(NO₂)C.tbd.CH, CH₂ CH(NO₂)C.tbd.CMe, CH₂ CO₂ Me, CH₂CO₂ Et, CH₂ CO₂ Pr-n, CH₂ CO₂ Pr-iso, CH₂ CO₂ Bu-n, CHMeCO₂ Me, CHMeCO₂Et, CH₂ CH₂ CO₂ Me, CH₂ CH₂ CO₂ Et, CH₂ CHMeCO₂ Me, CH₂ CH₂ CH₂ CO₂ Me,CH₂ CH═CHCO₂ Me, CH₂ CH═CHCO₂ Et, CH₂ CH═CHCO₂ Pr-n, CH₂ CH═CMeCO₂ Me,CH₂ CMe═CHCO₂ Me, CHMeCH═CHCO.sub. 2 Me, CHMeCH═CHCO₂ Et, CH₂ CH₂CH═CHCO₂ Me, CH₂ CH═CHCH₂ CO₂ Me, CH₂ C.tbd.CCO₂ Me, CH₂ C.tbd.CCO₂ Et,CH₂ C.tbd.CCO₂ Pr-n, CH₂ CH₂ C.tbd.CCO₂ Me, CH₂ CHMeC.tbd.CCO₂ Me, CH₂CMe₂ C.tbd.CCO₂ Me, CH₂ C.tbd.CCH₂ CO₂ Me, CH₂ COMe, CH₂ COEt, CH₂COPr-n, CH₂ CH₂ COMe, CH₂ CH₂ COEt, CH₂ CHMeCOMe, CH₂ CMe₂ COMe, CH₂COCF₃, CH₂ COCCl₃, CH₂ CH₂ COCF₃, CH₂ COCH₂ CF₃, CH₂ COCH₂ CHF₂, CH₂COCH₂ CHCl₂, CH₂ COCH₂ F, CH₂ COCH₂ Cl, CH₂ COCH₂ Br, CH₂ COCH═CH₂, CH₂COCH═CHMe, CH₂ COCH₂ CH═CH₂, CH₂ CH₂ COCH═CH₂, CH₂ CH₂ COCH═CHMe, CH₂COC.tbd.CH, CH₂ COC.tbd.CMe, CH₂ COCH₂ C.tbd.CH, CH₂ CH₂ COC.tbd.CH, CH₂CH₂ COC.tbd.CMe, CH₂ COCH₂ OMe, CH₂ COCH₂ OEt, CH₂ COCH₂ CH₂ OMe, CH₂COCH₂ CH₂ OEt, CH₂ CH₂ COCH₂ OMe, CH₂ CH₂ COCH₂ OEt, CH₂ COCH₂ SMe, CH₂COCH₂ SEt, CH₂ COCH₂ CH₂ SMe, CH₂ COCH₂ CH₂ SEt, CH₂ CH₂ COCH₂ SMe, CH₂CH₂ COCH₂ SEt, CH₂ COCH₂ SOMe, CH₂ COCH₂ SOEt, CH₂ COCH₂ CH₂ SOMe, CH₂COCH₂ CH₂ SOEt, CH₂ CH₂ COCH₂ SOMe, CH₂ CH₂ COCH₂ SOEt, CH₂ COCH₂ SO₂Me, CH₂ COCH₂ SO₂ Et, CH₂ COCH₂ CH₂ SO₂ Me, CH₂ COCH₂ CH₂ SO₂ Et, CH₂CH₂ COCH₂ SO₂ Me, CH₂ CH₂ COCH₂ SO₂ Et, CH₂ CH═CHCOMe, CH₂ CH═CHCOEt,CHMeCH═CHCOMe, CHMeCH═CHCOEt, CH₂ C.tbd.CCOMe, CH₂ C.tbd.CCOEt,CHMeC.tbd.CCOMe, CHMeC.tbd.CCOEt, CH₂ SO₂ NHMe, CH₂ SO₂ NHEt, CH₂ SO₂NHPr-n, CH₂ CH₂ SO₂ NHMe, CH₂ CH₂ SO₂ NHEt, CH₂ CH₂ SO₂ NHPr-n, CH₂ SO₂NHOMe, CH₂ SO₂ NHOEt, CH₂ SO₂ NHOPr-n, CH₂ CH₂ SO₂ NHOMe, CH₂ CH₂ SO₂NHOEt, CH₂ CH₂ SO₂ NHOPr-n, CH₂ SO₂ NMe₂, CH₂ SO₂ NMeEt, CH₂ SO₂ NEt₂,CH₂ CH₂ SO₂ NMe₂, CH₂ CH₂ SO₂ NMeEt, CH₂ CH₂ SO₂ NEt₂, CH₂ SO₂ N(OMe)Me,CH₂ SO₂ N(OMe)Et, CH₂ SO₂ N(OEt)Me, CH₂ CH₂ SO₂ N(OMe)Me, CH₂ CH₂ SO₂N(OMe)Et, CH₂ CH₂ SO₂ N(OEt)Me, CH₂ SO₂ N(OEt)Et, CH₂ CH₂ SO₂ N(OEt)Et,CH₂ CONHMe, CH₂ CONHEt, CH₂ CONHPr-n, CH₂ CH₂ CONHMe, CH₂ CH₂ CONHEt,CH₂ CH₂ CONHPr-n, CH₂ CONMe₂, CH₂ CONMeEt, CH₂ CONEt₂, CH₂ CH₂ CONMe₂,CH₂ CH₂ CONMeEt, CH₂ CH₂ CONEt₂, CH₂ CONHOMe, CH₂ CONHOEt, CH₂CONHOPr-n, CH₂ CH₂ CONHOMe, CH₂ CH₂ CONHOEt, CH₂ CH₂ CONHOPr-n, CH₂CON(OMe)Me, CH₂ CON(OMe)Et, CH₂ CON(OEt)Me, CH₂ CH₂ CON(OMe)Me, CH₂ CH₂CON(OMe)Et, CH₂ CON(OEt)Me, CH₂ CON(OEt)Et, CH₂ CH₂ CON(OEt)Et, CH₂NHMe, CH₂ NHEt, CH₂ NHPr-n, CH₂ CH₂ NHMe, CH₂ CH₂ NHEt, CH₂ CH₂ NHPr-n,CH₂ CHMeNHMe, CH₂ CHMeNHEt, CH₂ CHMeNHPr-n, CH₂ CH₂ CH₂ NHMe, CH₂ NHOMe,CH₂ NHOEt, CH₂ NHOPr-n, CH₂ CH₂ NHOMe, CH₂ CH₂ NHOEt, CH₂ CH₂ NHOPr-n,CH₂ CHMeNHOMe, CH₂ CHMeNHOEt, CH₂ CHMeNHOPr-n, CH₂ NMe₂, CH₂ NMeEt, CH₂NMePr-n, CH₂ CH₂ NMe₂, CH₂ CH₂ NMeEt, CH₂ CH₂ NMePr-n, CH₂ NEt₂, CH₂ CH₂NEt₂, CH₂ N(OMe)Me, CH₂ N(OMe)Et, CH₂ N(OEt)Me, CH₂ N(OEt)Et, CH₂ CH₂N(OMe)Me, CH₂ CH₂ N(OMe)Et, CH₂ CH₂ N(OEt)Me, CH₂ CH₂ N(OEt)Et, CH₂NMeCOMe, CH₂ NEtCOMe, CH₂ NMeCOEt, CH₂ CH₂ NMeCOMe, CH₂ CH₂ NEtCOMe, CH₂CH₂ NMeCOEt, CH₂ N(OMe)COMe, CH₂ N(OEt)COMe, CH₂ N(OMe)COEt, CH₂ CH₂N(OMe)COMe, CH₂ CH₂ N(OEt)COMe, CH₂ CH₂ N(OMe)COEt, CH₂ NMeSO₂ Me, CH₂NEtSO₂ Me, CH₂ NMeSO₂ Et, CH₂ CH₂ NMeSO₂ Me, CH₂ CH₂ NEtSO₂ Me, CH₂ CH₂NMeSO₂ Et, CH₂ N(OMe)SO₂ Me, CH₂ N(OEt)SO₂ Me, CH₂ N(OMe)SO₂ Et, CH₂ CH₂N(OMe)SO₂ Me, CH₂ CH₂ N(OEt)SO₂ Me, CH₂ CH₂ N(OMe)SO₂ Et, CH₂ Ph, CH₂CH₂ Ph, CH₂ CH₂ CH₂ Ph, CHMePh, CH₂ CHMePh, CH₂ CMe₂ Ph, CH₂ CH═CHPh,CH₂ CH═CMePh, CHMeCH═CHPh, CH₂ CMe═CMePh, CHMeCMe═CMePh, CH₂ C.tbd.CPh,CHMeC.tbd.CPh, CH₂ CMe₂ C.tbd.CPh, CH₂ CH₂ OPh, CH₂ CHMeOPh, CH₂ CMe₂OPh, CH₂ OPh, CH₂ CH₂ SPh, CH₂ CHMeSPh, CH₂ CMe₂ SPh, CH₂ SPh, CH₂ CH₂SOPh, CH₂ CHMeSOPh, CH₂ CMe₂ SOPh, CH₂ CH₂ SO₂ Ph, CH₂ CHMeSO₂ Ph, CH₂CMe₂ SO₂ Ph, CH₂ OCH₂ Ph, CH₂ CH₂ OCH₂ Ph, CH₂ CHMeOCH₂ Ph, CH₂ SCH₂ Ph,CH₂ CH₂ SCH₂ Ph, CH₂ CHMeSCH₂ Ph, CH₂ SOCH₂ Ph, CH₂ CH₂ SOCH₂ Ph, CH₂CHMeSOCH₂ Ph, CH₂ SO₂ CH₂ Ph, CH₂ CH₂ SO₂ CH₂ Ph, CH₂ CHMeSO₂ CH₂ Ph,CH₂ COPh, CH₂ CH₂ COPh, CHMeCOPh, CH₂ COCH₂ Ph, CH₂ CH₂ COCH₂ Ph,CHMeCOCH₂ Ph, CH₂ C(Cl)═CH₂, Ph, CH₂ SOPh, CH₂ SO₂ Ph, CH₂ C(Cl)═CHCl,CH₂ CH═C(I)Me, CH₂ CH═CHI, CH₂ C(F)═CHCl, CH₂ CH═CBr₂, CH₂ CH═CHF, CH₂C(Cl)═CHMe, CH₂ C(F)═CHBr, CH₂ C(Br)═CHCl, CH₂ C(Br)═CCl₂, CH₂ CH═CHCH₂F, CH₂ C(Br)═CH₂, CH₂ C(I)═CH₂, CH₂ C(Br)═C(Cl)Me, CH₂ C(I)═CHMe, CH₂C(Cl)═CCl₂, CH₂ CH═CHCCl₃, CH₂ C(Br)═CHMe, CH₂ C(Cl)═CHF, CH₂ C(Br)═CHF,CH₂ CH═C(Cl)Br, CH₂ C(F)═C(Cl)CF₃, CH₂ C(Cl)═C(Cl)Me, CH₂ C(Br)═CHBr,CH₂ CH═C(F)CF₂ Cl, CH₂ C(Br)═C(Br)Me, CH₂ CH═C(F)CF₃, CH₂ CH═CCl₂, CH₂C(F)═CH₂, CH₂ CH═CHCCl₃, CH₂ CH═C(F)Cl, CH₂ C(Cl)═C(F)Cl, CH₂ C(F)═CCl₂,CH₂ C(Cl)═CF₂, CH₂ C(CF₃)═CH₂, CMe₂ CH═CH₂, CMe₂ C.tbd.CH, CH₂ CH₂ I,CH₂ C.tbd.C-CN, CH₂ NHBu-n, CH₂ NHSO₂ Me, CH₂ NHSO₂ Et, CH₂ CH₂ NHSO₂Me, CH₂ CH₂ NHSO₂ Et, CH₂ NHCOMe, CH₂ NHCOEt, CH₂ CH₂ NHCOMe, CH₂ CH₂NHCOEt

Specific examples for the substituents R^(c2), R^(c3), R^(c4), R^(c5),R^(c6), R^(c11), and R^(c12) of the compound of the present invention

H, Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, Pen-n, Hex-n,Hep-n, CH═CH₂, CH═CHMe, CMe═CH₂, CH═CMe₂, CH═CHEt, CMe═CHMe, CMe═CMe₂,CH₂ CH═CH₂, CH₂ CH═CHMe, CHMeCH═CH₂, CMe₂ CH═CH₂, C.tbd.CH, C.tbd.CMe,C.tbd.CEt, CH₂ C.tbd.CH, CHMeC.tbd.CH, CMe₂ C.tbd.CH, Ph

Specific examples for the substituents R^(c7), R^(c8), R^(c9), R^(c10),R^(c13), and R^(c14) of the compound of the present invention

H, Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, Pen-n, Hex-n,CH₂ F, CHF₂, CF₃, CH₂ Cl, CH₂ Br, CH₂ CF₃, CH₂ CH₂ F, CH₂ CH₂ Cl, CH₂CH₂ Br, CF₂ CF₃, OMe, OEt, OPr-n, OPr-iso, OCF₃, OCH₂ CF₃, SMe, SEt,SPr-n, SPr-iso, SOMe, SOEt, SOPr-n, SOPr-iso, SO₂ Me, SO₂ Et, SO₂ Pr-n,SO₂ Pr-iso, CO₂ Me, CO₂ Et, CO₂ Pr-n, CO₂ Pr-iso, CO₂ Bu-n, COMe, COEt,COPr-n, COPr-iso, COBu-n, F, Cl, Br, I, NO₂, CN, Ph

Specific examples for the substituents R^(d2), R^(d3) and R^(d4) of thecompound of the present invention

H, Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, Pen-n, Hex-n,Hep-n, CH═CH₂, CH═CHMe, CH═CHEt, CMe═CH₂, CH═CMe₂, CMe═CHMe, CMe═CMe₂,CH₂ CH═CH₂, CH₂ CH═CHMe, CHMeCH═CH₂, CHMeCH═CHMe, CMe₂ CH═CH₂, CMe₂CH═CHMe, C.tbd.CH, C.tbd.CMe, C.tbd.CEt, CH₂ C.tbd.CH, CH₂ C.tbd.CMe,CHMeC.tbd.CH, CHMeC.tbd.CMe, CMe₂ C.tbd.CH, CMe₂ C.tbd.CMe, Ph

Specific examples for the substituent R^(d5) of the compound of thepresent invention

Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, Pen-n, Hex-n,Hep-n, CH₂ CH═CH₂, CH₂ CH═CHMe, CH₂ CH═CHEt, CH₂ CH₂ CH═CH₂, CH₂ CH₂CH═CHMe, CH₂ CH═CMe₂, CHMeCH═CH₂, CH₂ CMe═CH₂, CH₂ CMe═CHMe,CHMeCH═CHMe, CH₂ CMe═CHEt, CH₂ CH₂ CH═CMe₂, CH₂ CMe═CMe₂, CMe₂ CH═CH₂,CMe₂ CH═CHMe, CH₂ C.tbd.CH, CH₂ C.tbd.CMe, CH₂ C.tbd.CEt, CH₂ CH₂C.tbd.CH, CH₂ CH₂ C.tbd.CMe, CHMeC.tbd.CH, CHMeC.tbd.CMe, CMe₂ C.tbd.CH,CMe₂ C.tbd.CMe, Ph

Specific examples for the substituents R^(d6) and R^(f2) of the compoundof the present invention

Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, Pen-n, Hex-n,Hep-n, CH₂ CH═CH₂, CH₂ CH═CHMe, CH₂ CH═CHEt, CH₂ CH₂ CH═CH₂, CH₂ CH₂CH═CHMe, CH₂ CH═CMe₂, CHMeCH═CH₂, CH₂ CMe═CH₂, CH₂ CMe═CHMe,CHMeCH═CHMe, CH₂ CMe═CHEt, CH₂ CH₂ CH═CMe₂, CH₂ CMe═CMe₂, CMe₂ CH═CH₂,CMe₂ CH═CHMe, CH₂ C.tbd.CH, CH₂ C.tbd.CMe, CH₂ C.tbd.CEt, CH₂ CH₂C.tbd.CH, CH₂ CH₂ C.tbd.CMe, CHMeC.tbd.CH, CHMeC.tbd.CMe, CMe₂ C.tbd.CH,CMe₂ C.tbd.CMe, CH₂ SMe, CH₂ SEt, CH₂ SPr-n, CH₂ SBu-n, CH₂ CH₂ SMe, CH₂CH₂ SEt, CH₂ CH₂ SPr-n, CH₂ SOMe, CH₂ SOEt, CH₂ SOPr-n, CH₂ CH₂ SOMe,CH₂ CH₂ SOEt, CH₂ CH₂ SOPr-n, CH₂ SO₂ Me, CH₂ SO₂ Et, CH₂ SO₂ Pr-n, CH₂SO₂ Bu-n, CH₂ CH.sub. 2 SO₂ Me, CH₂ CH₂ SO₂ Et, CH₂ CH₂ SO₂ Pr-n, CH₂OMe, CH₂ OEt, CH₂ OPr-n, CH₂ OBu-n, CH₂ CH₂ OMe, CH₂ CH₂ OEt, CH₂ CH₂OPr-n, CH₂ CO₂ Me, CH₂ CO₂ Et, CH₂ CO₂ Pr-n, CH₂ CO₂ Bu-n, CHMeCO₂ Me,CHMeCO₂ Et, CHMeCO₂ Pr-n, CMe₂ CO₂ Me, CMe₂ CO₂ Et, CH₂ COMe, CH₂ COEt,CH₂ COPr-n, CH₂ COBu-n, CH₂ CH₂ COMe, CH₂ CH₂ COEt, CH₂ CH₂ COPr-n, CH₂CN, CH₂ CH₂ CN, CH₂ CH₂ CH₂ CN, Ph, CH₂ Ph, CH₂ CH₂ Ph, CHMePh

Specific examples for the substituents R^(e2), R^(e3), R^(e6) and R^(e7)of the compound of the present invention

H, Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, Pen-n, Hex-n,CH₂ F, CHF₂, CF₃, CH₂ Cl, CH₂ Br, CH₂ CF₃, CH₂ CH₂ F, CH₂ CH₂ Cl, CH₂CH₂ Br, CF₂ CF₃, OMe, OEt, OPr-n, OPr-iso, OCF₃, OCH₂ CF₃, SMe, SEt,SPr-n, SPr-iso, SOMe, SOEt, SOPr-n, SOPr-iso, SO₂ Me, SO₂ Et, SO₂ Pr-n,SO₂ Pr-iso, CO₂ Me, CO₂ Et, CO₂ Pr-n, CO₂ Pr-iso, CO₂ Bu-n, COMe, COEt,COPr-n, COPr-iso, COBu-n, F, Cl, Br, I, NO₂, CN, Ph

Specific examples for the substituents R^(e4), R^(e5), R^(e8), R^(e9)and R^(e10) of the compound of the present invention

H, Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, Pen-n, Hex-n,CH═CH₂, CH═CHMe, CH═CHEt, CMe═CH₂, CH═CMe₂, CMe═CHMe, CMe═CMe₂, CH₂CH═CH₂, CH₂ CH═CHMe, CHMeCH═CH₂, CHMeCH═CHMe, CMe₂ CH═CH₂, CMe₂ CH═CHMe,C.tbd.CH, C.tbd.CMe, C.tbd.CEt, CH₂ C.tbd.CH, CH₂ C.tbd.CMe,CHMeC.tbd.CH, CHMeC.tbd.CMe, CMe₂ C.tbd.CH, CMe₂ C.tbd.CMe, Ph

Specific examples for the substituents R^(f3), R^(f4), R^(f7), R^(f8),R^(f11) and R^(f12) of the compound of the present invention

H, Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, CH₂ F, CHF₂,CF₃, CH₂ Cl, CH₂ Br, CH₂ CF₃, CH₂ CH₂ F, CH₂ CH₂ Cl, CH₂ CH₂ Br, CF₂CF₃, OMe, OEt, OPr-n, OPr-iso, OCF₃, OCH₂ CF₃, SMe, SEt, SPr-n, SPr-iso,SOMe, SOEt, SOPr-n, SOPr-iso, SO₂ Me, SO₂ Et, SO₂ Pr-n, SO₂ Pr-iso, CO₂Me, CO₂ Et, CO₂ Pr-n, CO₂ Pr-iso, CO₂ Bu-n, COMe, COEt, COPr-n,COPr-iso, COBu-n, F, Cl, Br, I, NO₂, CN, Ph

Specific examples for the substituents R^(f5), R^(f6), R^(f9), R^(f10),R^(f13), R^(f14) and R^(f15) of the compound of the present invention

H, Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, Pen-n, Hex-n,Hep-n, CH═CH₂, CH═CHMe, CH═CHEt, CMe═CH₂, CH═CMe₂, CMe═CHMe, CMe═CMe₂,CH₂ CH═CH₂, CH₂ CH═CHMe, CHMeCH═CH₂, CHMeCH═CHMe, CMe₂ CH═CH₂, CMe₂CH═CHMe, C.tbd.CH, C.tbd.CMe, C.tbd.CEt, CH₂ C.tbd.CH, CH₂ C.tbd.CMe,CHMeC.tbd.CH, CHMeC.tbd.CMe, CMe₂ C.tbd.CH, CMe₂ C.tbd.CMe, Ph

Specific examples for the substituent R^(g1) of the compound of thepresent invention

Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, Pen-n, Hex-n,Hep-n, Pr-cyc, Bu-cyc, Pen-cyc, Hex-cyc, CH₂ Pr-cyc, CH₂ CH₂ Pr-cyc,CHMe-Pr-cyc, CH₂ CHMe-Pr-cyc, CHMeCH₂ Pr-cyc, CH₂ Bu-cyc, CH₂ CH₂Bu-cyc, CH₂ Pen-cyc, CH₂ Hex-cyc, ##STR6## CH₂ CH═CH₂, CH₂ CH═CHMe, CH₂CH═CHEt, CH₂ CH₂ CH═CH₂, CH₂ CH₂ CH═CHMe, CH₂ CH═CMe₂, CHMeCH═CH₂, CH₂CMe═CH₂, CH₂ CMe═CHMe, CHMeCH═CHMe, CH₂ CMe═CHEt, CH₂ CH₂ CH═CMe₂, CH₂CMe═CMe₂, CH₂ C.tbd.CH, CH₂ C.tbd.CMe, CH₂ C.tbd.CEt, CH₂ CH₂ C.tbd.CH,CH₂ CH₂ C.tbd.CMe, CHMeC.tbd.CH, CHMeC.tbd.CMe, CH₂ OMe, CH₂ OEt, CH₂OPr-n, CH₂ OPr-iso, CH₂ CH₂ OMe, CH₂ CH₂ OEt, CH₂ CH₂ OPr-n, CHMeOMe,CHMeOEt, CH₂ CHMeOMe, CH₂ CHMeOEt, CH₂ CH₂ CH₂ OMe, CH₂ CH₂ CH₂ OEt, CH₂OCH₂ CH═CH₂, CH₂ OCH₂ CH═CHMe, CH₂ CH₂ OCH₂ CH═CH₂, CH₂ CH₂ OCH₂CH═CHMe, CH₂ OCH₂ C.tbd.CH, CH₂ OCH₂ C.tbd.CMe, CH₂ OCHMeC.tbd.CH, CH₂OCMe₂ C.tbd.CH, CH₂ CH₂ OCH₂ C.tbd.CH, CH₂ CH₂ OCH₂ C.tbd.CMe, CH₂ CH₂OCHMeC.tbd.CH, CH₂ CH₂ OCMe₂ C.tbd.CH, CH₂ OCHF₂, CH₂ OCF₃, CH₂ OCF₂CF₃, CH₂ CH₂ OCHF₂, CH₂ CH₂ OCF₃, CH₂ CH₂ OCF₂ CF₃, CH₂ OCH₂ CF₃, CH₂CH₂ OCH₂ CF₃, CH₂ OCH₂ CHF₂, CH₂ CH₂ OCH₂ CHF₂, CH₂ OCH₂ CH₂ F, CH₂ OCH₂CH₂ Cl, CH₂ OCH₂ CH₂ Br, CH₂ CH₂ OCH₂ CH₂ F, CH₂ CH₂ OCH₂ CH₂ Cl, CH₂CH₂ OCH₂ CH₂ Br, CH₂ OCH₂ CH═CHCl, CH₂ CH₂ OCH₂ CH═CHCl, CH₂ OCH₂CH═CHBr, CH₂ CH₂ OCH₂ CH═CHBr, CH₂ OCH₂ CF═CF₂, CH₂ CH₂ OCH₂ CF═CF₂, CH₂OCH═CHCl, CH₂ CH₂ OCH═CHCl, CH₂ OCF═CF₂, CH₂ CH₂ OCF═CF₂, CH₂ OCF₂CF═CF₂, CH₂ CH₂ OCF₂ CF═CF₂, CH₂ OCH₂ CH═CF.sub. 2, CH₂ CH₂ OCH₂ CH═CF₂,CH₂ OCH₂ CH═CHCF₃, CH₂ CH₂ OCH₂ CH═CHCF₃, CH₂ OCH₂ C.tbd.CI, CH₂ OCH₂CH₂ C.tbd.CI, CH₂ CH₂, OCH₂ C.tbd.CI, CH₂ OCH₂ C.tbd.CCF₃, CH₂ CH₂ OCH₂C.tbd.CCF₃, CH₂ OCMe₂ C.tbd.CI, CH₂ CH₂ OCMe₂ C.tbd.CI, CH₂ OCMe₂C.tbd.CCF₃, CH₂ CH₂ OCMe₂ C.tbd.CCF₃, CH₂ SMe, CH₂ SEt, CH₂ SPr-n, CH₂CH₂ SMe, CH₂ CH₂ SEt, CH₂ CH₂ SPr-n, CHMeSMe, CHMeSEt, CH₂ CHMeSMe, CH₂CHMeSEt, CH₂ SOMe, CH₂ SOEt, CH₂ SOPr-n, CH₂ CH₂ SOMe, CH₂ CH₂ SOEt, CH₂CH₂ SOPr-n, CHMeSOMe, CHMeSOEt, CH₂ CHMeSOMe, CH₂ CHMeSOEt, CH₂ SO₂ Me,CH₂ SO₂ Et, CH₂ SO₂ Pr-n, CH₂ CH₂ SO₂ Me, CH₂ CH₂ SO₂ Et, CH₂ CH₂ SO₂Pr-n, CHMeSO₂ Me, CHMeSO₂ Et, CH₂ CHMeSO₂ Me, CH₂ CHMeSO₂ Et, CH₂ CH₂ F,CH₂ CHF₂, CH₂ CF₃, CH.sub. 2 CH₂ Cl, CH₂ CH₂ Br, CH₂ CCl₃, CH₂ CH₂ CF₃,CH₂ CH₂ CCl₃, CH₂ CH₂ CH₂ F, CH₂ CH₂ CH₂ Cl, CF₂ CF₃, CH₂ CF₂ CF₃, CH₂CH═CHCl, CH₂ CH═CHBr, CH₂ CH═CF₂, CH₂ CF═CF₂, CH₂ CH═CHCF₃, CH₂CH═CBrMe, CH₂ CH═CClMe, CH₂ CH═C(CF₃)Me, CF₂ CF═CF₂, CH₂ C.tbd.CI, CH₂CH₂ C.tbd.CI, CH₂ C.tbd.CCF₃, CH₂ CH₂ C.tbd.CCF₃, CH₂ CN, CH₂ CH₂ CN,CHMeCN, CH₂ CHMeCN, CH₂ CMe₂ CN, CH₂ CH═CHCN, CH₂ CH(CN)CH═CH₂, CH₂C(CN)═CH₂, CH₂ C(CN)═CHMe, CH₂ CH(CN)C.tbd.CH, CH₂ CH(CN)C.tbd.C-Me,CH(CN)C.tbd.CH, CH₂ NO₂, CH₂ CH₂ NO₂, CH₂ CHMeNO₂, CH₂ CMe₂ NO₂, CH₂ CH₂CH.sub. 2 NO₂, CH₂ CH═CHNO₂, CH₂ CH(NO₂)CH═CH₂, CH₂ C(NO₂)═CH₂, CH₂C(NO₂)═CHMe, CH₂ CH(NO₂)C.tbd.CH, CH₂ CH(NO₂)C.tbd.CMe, CH₂ CO₂ Me, CH₂CO₂ Et, CH₂ CO₂ Pr-n, CH₂ CO₂ Pr-iso, CH₂ CO₂ Bu-n, CHMeCO₂ Me, CHMeCO₂Et, CH₂ CH₂ CO₂ Me, CH₂ CH₂ CO₂ Et, CH₂ CHMeCO₂ Me, CH₂ CH₂ CH₂ CO₂ Me,CH₂ CH═CHCO₂ Me, CH₂ CH═CHCO₂ Et, CH₂ CH═CHCO₂ Pr-n, CH₂ CH═CMeCO₂ Me,CH₂ CMe═CHCO₂ Me, CHMeCH═CHCO₂ Me, CHMeCH═CHCO₂ Et, CH₂ CH₂ CH═CHCO₂ Me,CH₂ CH═CHCH₂ CO₂ Me, CH₂ C.tbd.CCO₂ Me, CH₂ C.tbd.CCO₂ Et, CH₂C.tbd.CCO₂ Pr-n, CH₂ CH₂ C.tbd.CCO₂ Me, CH₂ CHMeC.tbd.CCO₂ Me, CH₂ CMe₂C.tbd.CCO₂ Me, CH₂ C.tbd.CCH₂ CO₂ Me, CH₂ COMe, CH₂ COEt, CH₂ COPr-n,CH₂ CH.sub. 2 COMe, CH₂ CH₂ COEt, CH₂ CHMeCOMe, CH₂ CMe₂ COMe, CH₂COCF₃, CH₂ COCCl₃, CH₂ CH₂ COCF₃, CH₂ COCH₂ CF₃, CH₂ COCH₂ CHF₂, CH₂COCH₂ CHCl₂, CH₂ COCH₂ F, CH₂ COCH₂ Cl, CH₂ COCH₂ Br, CH₂ COCH═CH₂, CH₂COCH═CHMe, CH₂ COCH₂ CH═CH₂, CH₂ CH₂ COCH═CH₂, CH₂ CH₂ COCH═CHMe, CH₂COC.tbd.CH, CH₂ COC.tbd.CMe, CH₂ COCH₂ C.tbd.CH, CH₂ CH₂ COC.tbd.CH, CH₂CH₂ COC.tbd.CMe, CH₂ COCH₂ OMe, CH₂ COCH₂ OEt, CH₂ COCH₂ CH₂ OMe, CH₂COCH₂ CH₂ OEt, CH₂ CH₂ COCH₂ OMe, CH₂ CH₂ COCH₂ OEt, CH₂ COCH₂ SMe, CH₂COCH₂ SEt, CH₂ COCH₂ CH₂ SMe, CH₂ COCH₂ CH₂ SEt, CH₂ CH₂ COCH₂ SMe, CH₂CH₂ COCH₂ SEt, CH₂ COCH₂ SOMe, CH₂ COCH₂ SOEt, CH₂ COCH₂ CH₂ SOMe, CH₂COCH₂ CH₂ SOEt, CH₂ CH₂ COCH₂ SOMe, CH₂ CH₂ COCH₂ SOEt, CH₂ COCH₂ SO₂Me, CH₂ COCH₂ SO₂ Et, CH₂ COCH₂ CH₂ SO₂ Me, CH₂ COCH₂ CH₂ SO₂ Et, CH₂CH₂ COCH₂ SO₂ Me, CH₂ CH₂ COCH₂ SO₂ Et, CH₂ CH═CHCOMe, CH₂ CH═CHCOEt,CHMeCH═CHCOMe, CHMeCH═CHCOEt, CH₂ C.tbd.CCOMe, CH₂ C.tbd.CCOEt,CHMeC.tbd.CCOMe, CHMeC.tbd.CCOEt, CH₂ SO₂ NHMe, CH₂ SO₂ NHEt, CH₂ SO₂NHPr-n, CH₂ CH₂ SO₂ NHMe, CH₂ CH₂ SO₂ NHEt, CH₂ CH₂ SO₂ NHPr-n, CH₂ SO₂NHOMe, CH₂ SO₂ NHOEt, CH₂ SO₂ NHOPr-n, CH₂ CH₂ SO₂ NHOMe, CH₂ CH₂ SO₂NHOEt, CH₂ CH₂ SO₂ NHOPr-n, CH₂ SO₂ NMe₂, CH.sub. 2 SO₂ NMeEt, CH₂ SO₂NEt₂, CH₂ CH₂ SO₂ NMe₂, CH₂ CH₂ SO₂ NMeEt, CH₂ CH₂ SO₂ NEt₂, CH₂ SO₂N(OMe)Me, CH₂ SO₂ N(OMe)Et, CH₂ SO₂ N(OEt)Me, CH₂ CH₂ SO₂ N(OMe)Me, CH₂CH₂ SO₂ N(OMe)Et, CH₂ CH₂ SO₂ N(OEt)Me, CH₂ SO₂ N(OEt)Et, CH₂ CH₂ SO₂N(OEt)Et, CH₂ CONHMe, CH₂ CONHEt, CH₂ CONHPr-n, CH₂ CH₂ CONHMe, CH₂ CH₂CONHEt, CH₂ CH₂ CONHPr-n, CH₂ CONMe₂, CH₂ CONMeEt, CH₂ CONEt₂, CH₂ CH₂CONMe₂, CH₂ CH₂ CONMeEt, CH₂ CH₂ CONEt₂, CH₂ CONHOMe, CH₂ CONHOEt, CH₂CONHOPr-n, CH₂ CH₂ CONHOMe, CH₂ CH₂ CONHOEt, CH₂ CH₂ CONHOPr-n, CH₂CON(OMe)Me, CH₂ CON(OMe)Et, CH₂ CON(OEt)Me, CH₂ CH₂ CON(OMe)Me, CH₂ CH₂CON(OMe)Et, CH₂ CH₂ CON(OEt)Me, CH₂ CON(OEt)Et, CH₂ CH₂ CON(OEt)Et, CH₂NHMe, CH₂ NHEt, CH₂ NHPr-n, CH₂ CH₂ NHMe, CH₂ CH₂ NHEt, CH₂ CH₂ NHPr-n,CH₂ CHMeNHMe, CH₂ CHMeNHEt, CH₂ CHMeNHPr-n, CH₂ CH₂ CH₂ NHMe, CH₂ NHOMe,CH₂ NHOEt, CH₂ NHOPr-n, CH₂ CH₂ NHOMe, CH₂ CH₂ NHOEt, CH₂ CH₂ NHOPr-n,CH₂ CHMeNHOMe, CH₂ CHMeNHOEt, CH₂ CHMeNHOPr-n, CH₂ NMe₂, CH₂ NMeEt, CH₂NMePr-n, CH₂ CH₂ NMe₂, CH₂ CH₂ NMeEt, CH₂ CH₂ NMePr-n, CH₂ NEt₂, CH₂ CH₂NEt₂, CH₂ N(OMe)Me, CH₂ N(OMe)Et, CH₂ N(OEt)Me, CH₂ N(OEt)Et, CH₂ CH₂N(OMe)Me, CH₂ CH₂ N(OMe)Et, CH₂ CH₂ N(OEt)Me, CH₂ CH₂ N(OEt)Et, CH₂NMeCOMe, CH₂ NEtCOMe, CH₂ NMeCOEt, CH₂ CH₂ NMeCOMe, CH₂ CH₂ NEtCOMe, CH₂CH.sub. 2 NMeCOEt, CH₂ N(OMe)COMe, CH₂ N(OEt)COMe, CH₂ N(OMe)COEt, CH₂CH₂ N(OMe)COMe, CH₂ CH₂ N(OEt)COMe, CH₂ CH₂ N(OMe)COEt, CH₂ NMeSO₂ Me,CH₂ NEtSO₂ Me, CH₂ NMeSO₂ Et, CH₂ CH₂ NMeSO₂ Me, CH₂ CH₂ NEtSO₂ Me, CH₂CH₂ NMeSO₂ Et, CH₂ N(OMe)SO₂ Me, CH₂ N(OEt)SO₂ Me, CH₂ N(OMe)SO₂ Et, CH₂CH₂ N(OMe)SO₂ Me, CH₂ CH₂ N(OEt)SO₂ Me, CH₂ CH₂ N(OMe)SO₂ Et, CH₂ Ph,CH₂ CH₂ Ph, CH₂ CH₂ CH₂ Ph, CHMePh, CH₂ CHMePh, CH₂ CMe₂ Ph, CH₂CH═CHPh, CH₂ CH═CMePh, CHMeCH═CHPh, CH₂ CMe═CMePh, CHMeCMe═CMePh, CH₂C.tbd.CPh, CHMeC.tbd.CPh, CH₂ CMe₂ C.tbd.CPh, CH₂ CH₂ OPh, CH₂ CHMeOPh,CH₂ CMe₂ OPh, CH₂ OPh, CH₂ CH₂ SPh, CH₂ CHMeSPh, CH₂ CMe₂ SPh, CH₂ SPh,CH₂ CH₂ SOPh, CH₂ CHMeSOPh, CH₂ CMe₂ SOPh, CH₂ CH₂ SO₂ Ph, CH₂ CHMeSO₂Ph, CH₂ CMe₂ SO₂ Ph, CH₂ OCH₂ Ph, CH₂ CH₂ OCH₂ Ph, CH₂ CHMeOCH₂ Ph, CH₂SCH₂ Ph, CH₂ CH₂ SCH₂ Ph, CH₂ CHMeSCH₂ Ph, CH₂ SOCH₂ Ph, CH₂ CH₂ SOCH₂Ph, CH₂ CHMeSOCH₂ Ph, CH₂ SO₂ CH₂ Ph, CH₂ CH₂ SO₂ CH₂ Ph, CH₂ CHMeSO₂CH₂ Ph, CH₂ COPh, CH₂ CH₂ COPh, CHMeCOPh, CH₂ COCH₂ Ph, CH₂ CH.sub. 2COCH₂ Ph, CHMeCOCH₂ Ph

Specific examples for the substituents R^(g2) and R^(g3) of the compoundof the present invention

Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, Pen-n, Hex-n, CH₂CH═CH₂, CH₂ CH═CHMe, CH₂ CH═CHEt, CH₂ CH₂ CH═CH₂, CH₂ CH₂ CH═CHMe, CH₂CH═CMe₂, CHMeCH═CH₂, CH₂ CMe═CH₂, CH₂ CMe═CHMe, CHMeCH═CHMe, CH₂CMe═CHEt, CH₂ CH₂ CH═CMe₂, CH₂ CMe═CMe₂, CH₂ C.tbd.CH, CH₂ C.tbd.CMe,CH₂ C.tbd.CEt, CH₂ CH₂ C.tbd.CH, CH₂ CH₂ C.tbd.CMe, CHMeC.tbd.CH,CHMeC.tbd.CMe, CH₂ F, CHF₂, CF₃, CH₂ Cl, CH₂ Br, CH₂ CF₃, CH₂ CH₂ F, CH₂CH₂ Cl, CH₂ CH₂ Br, CF₂ CF₃, OMe, OEt, OPr-n, OPr-iso, SO₂ Me, SO₂ Et,SO₂ Pr-n, SO₂ Pr-iso, SO₂ NHMe, SO₂ NHEt, SO₂ NHPr-n, SO₂ NHPr-iso, SO₂NMe₂, SO₂ NEt₂, SO₂ N(Pr-n)₂, SO₂ NMeEt, SO₂ NMePr-n, CO₂ Me, CO₂ Et,CO₂ Pr-n, CO₂ Pr-iso, CO₂ Bu-n, COMe, COEt, COPr-n, COPr-iso, COBu-n,CONHMe, CONHEt, CONHPr-n, CONHPr-iso, CONMe₂, CONEt₂, CON(Pr-n)₂,CONMeEt, CONMePr-n, Ph, PhCH₂

Specific examples of --NR^(g2) R^(g3) wherein the substituents R^(g2)and R^(g3) of the compound of the present invention form a saturated 3-to 7-membered heterocyclic ring together with the nitrogen atom to whichthey are bonded ##STR7## Specific examples for the substituent L of thecompound of the present invention

H, Me, Et, Pr-n, CH₂ CH═CH₂, CH₂ C.tbd.CH

Specific examples for the substituents B and D of the compound of thepresent invention

Me, Et, Pr-n, OMe, OEt, CH₂ F, CHF₂, CF₃, OCHF₂, OCF₃, F, Cl, Br, NHMe,NHEt, NHPr-n, OCH₂ CF₃, NMe₂, OCBrF₂, CH₂ Cl, CH₂ F

Now, examples of the compound covered by the present invention will bepresented in the following Tables 1A, 1B, 1C, 2A, 2B, 2C, 3, 4A, 4B, 4C,5, 6, 7, 8, 9, 10, 11 and 12. However, the compound of the presentinvention is not limited to such examples. The symbols in these Tableshave the following meanings.

Me: methyl group, Et: ethyl group, Pr-n: n-propyl group, Pr-iso:isopropyl group, Bu-n: n-butyl group, Bu-iso: isobutyl group, Bu-sec:sec-butyl group, Bu-tert: tert-butyl group, Pen-n: n-pentyl group,Hex-n: n-hexyl group, Hep-n: n-heptyl group, Pr-cyc: cyclopropyl group,Bu-cyc: cyclobutyl group, Pen-cyc: cyclopentyl group, Hex-cyc:cyclohexyl group, and Ph: phenyl group, ##STR8## Gn is the same as aboveG and represents the following Ga, Gb and Gc. Ga=G1 to G90 (i.e.represents any one of G1 to G90)

Gb=G1 to G13 (i.e. represents any one of G1 to G13)

Gc=G1 to G6 (i.e. represents any one of G1 to G6) ##STR9##

                  TABLE 1A                                                        ______________________________________                                         ##STR10##                                                                     ##STR11##                                                                     ##STR12##                                                                     ##STR13##                                                                     ##STR14##                                                                     ##STR15##                                                                     ##STR16##                                                                     ##STR17##                                                                     ##STR18##                                                                     ##STR19##                                                                     ##STR20##                                                                     ##STR21##                                                                     ##STR22##                                                                     ##STR23##                                                                     ##STR24##                                                                     ##STR25##                                                                     ##STR26##                                                                     ##STR27##                                                                     ##STR28##                                                                     ##STR29##                                                                     ##STR30##                                                                     ##STR31##                                                                     ##STR32##                                                                     ##STR33##                                                                     ##STR34##                                                                     ##STR35##                                                                     ##STR36##                                                                     ##STR37##                                                                     ##STR38##                                                                     ##STR39##                                                                     ##STR40##                                                                     ##STR41##                                                                     ##STR42##                                                                     ##STR43##                                                                     ##STR44##                                                                     ##STR45##                                                                     ##STR46##                                                                     ##STR47##                                                                     ##STR48##                                                                     ##STR49##                                                                     ##STR50##                                                                     ##STR51##                                                                     ##STR52##                                                                     ##STR53##                                                                     ##STR54##                                                                    R.sup.m                   Gn                                                  ______________________________________                                        Me                        Ga                                                  Et                        Ga                                                  Pr-n                      Ga                                                  Pr-iso                    Ga                                                  Bu-n                      Ga                                                  Bu-iso                    Ga                                                  Bu-sec                    Gb                                                  Bu-tert                   Gb                                                  Pen-n                     Ga                                                  Hex-n                     Gb                                                  Hep-n                     Gb                                                  Pr-cyc                    Ga                                                  Hex-cyc                   Ga                                                  CH.sub.2 Pr-cyc           Ga                                                  CH.sub.2 CH.sub.2 Pr-cyc  Ga                                                  CH.sub.2 Bu-cyc           Gb                                                  CH.sub.2 Pen-cyc          Gc                                                  Hexen-cyc                 Gb                                                  CH.sub.2 Penten-cyc       Gb                                                  CH.sub.2 CHCH.sub.2       Ga                                                  CH.sub.2 CHCHMe           Ga                                                  CH.sub.2 CHCHEt           Ga                                                  CH.sub.2 CHCMe.sub.2      Gb                                                  CH.sub.2 CMeCH.sub.2      Ga                                                  CH.sub.2 CHMeCHCHMe       Gc                                                  CH.sub.2 CH.sub.2 CHCH.sub.2                                                                            Ga                                                  CH.sub.2 CH.sub.2 CHCHMe  Gb                                                  CH.sub.2 CCH              Ga                                                  CH.sub.2 CCMe             Ga                                                  CH.sub.2 CCEt             Ga                                                  CH.sub.2 CH.sub.2 CCH     Ga                                                  CH.sub.2 CH.sub.2 CCMe    Gb                                                  CHMeCCH                   Gb                                                  CHMeCCMe                  Gc                                                  CH.sub.2 OMe              Ga                                                  CH.sub.2 OEt              Ga                                                  CH.sub.2 OPr-n            Gb                                                  CH.sub.2 CH.sub.2 OMe     Ga                                                  CH.sub.2 CH.sub.2 OEt     Ga                                                  CH.sub.2 CH.sub.2 OPr-n   Gb                                                  CH.sub.2 CHMeOMe          Gb                                                  CH.sub.2 CH.sub.2 CH.sub.2 OMe                                                                          Ga                                                  CH.sub.2 CH.sub.2 CH.sub.2 OEt                                                                          Ga                                                  CH.sub.2 OCH.sub.2 CHCH.sub.2                                                                           Ga                                                  CH.sub.2 OCH.sub.2 CHCHMe Ga                                                  CH.sub.2 CH.sub.2 OCH.sub.2 CHCH.sub.2                                                                  Ga                                                  CH.sub.2 CH.sub.2 OCH.sub.2 CHCHMe                                                                      Ga                                                  CH.sub.2 OCH.sub.2 CCH    Ga                                                  CH.sub.2 OCH.sub.2 CCMe   Ga                                                  CH.sub.2 CH.sub.2 OCH.sub.2 CCH                                                                         Ga                                                  CH.sub.2 CH.sub.2 OCH.sub.2 CCMe                                                                        Ga                                                  CH.sub.2 OCHF.sub.2       Ga                                                  CH.sub.2 OCF.sub.3        Ga                                                  CH.sub.2 CH.sub.2 OCHF.sub.2                                                                            Ga                                                  CH.sub.2 CH.sub.2 OCF.sub.3                                                                             Ga                                                  CH.sub.2 OCH.sub.2 CF.sub.3                                                                             Ga                                                  CH.sub.2 CH.sub.2 OCH.sub.2 CF.sub.3                                                                    Ga                                                  CH.sub.2 OCH.sub.2 CH.sub.2 F                                                                           Ga                                                  CH.sub.2 OCH.sub.2 CH.sub.2 Cl                                                                          Ga                                                  CH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 F                                                                  Ga                                                  CH.sub. 2 CH.sub.2 OCH.sub.2 CH.sub.2 Cl                                                                Ga                                                  CH.sub.2 OCH.sub.2 CHCHCl Gb                                                  CH.sub.2 CH.sub.2 OCH.sub.2 CHCHCl                                                                      Gb                                                  CH.sub.2 OCH.sub.2 CHCHBr Gb                                                  CH.sub.2 CH.sub.2 OCH.sub.2 CHCHBr                                                                      Gb                                                  CH.sub.2 OCH.sub.2 CHCF.sub.2                                                                           Gb                                                  CH.sub.2 CH.sub.2 OCH.sub.2 CHCF.sub.2                                                                  Gb                                                  CH.sub.2 OCH.sub.2 CHCHCF.sub.3                                                                         Gb                                                  CH.sub.2 CH.sub.2 OCH.sub.2 CHCHCF.sub.3                                                                Gb                                                  CH.sub.2 OCH.sub.2 CCI    Gb                                                  CH.sub.2 CH.sub.2 OCH.sub.2 CCI                                                                         Gb                                                  CH.sub.2 OCH.sub.2 CCCF.sub.3                                                                           Gb                                                  CH.sub.2 CH.sub.2 OCH.sub.2 CCCF.sub.3                                                                  Gb                                                  CH.sub.2 SMe              Ga                                                  CH.sub.2 SEt              Ga                                                  CH.sub.2 SPr-n            Gb                                                  CH.sub.2 CH.sub.2 SMe     Ga                                                  CH.sub.2 CH.sub.2 SEt     Ga                                                  CH.sub.2 CH.sub.2 SPr-n   Gb                                                  CH.sub.2 SOMe             Gb                                                  CH.sub.2 SOEt             Gb                                                  CH.sub.2 CH.sub.2 SOMe    Gb                                                  CH.sub.2 CH.sub.2 SOEt    Gb                                                  CH.sub.2 SO.sub.2 Me      Ga                                                  CH.sub.2 SO.sub.2 Et      Ga                                                  CH.sub.2 SO.sub.2 Pr-n    Gb                                                  CH.sub.2 CH.sub.2 SO.sub.2 Me                                                                           Ga                                                  CH.sub.2 CH.sub.2 SO.sub.2 Et                                                                           Ga                                                  CH.sub.2 CH.sub.2 SO.sub.2 Pr-n                                                                         Gb                                                  CH.sub.2 CH.sub.2 F       Ga                                                  CH.sub.2 CHF.sub.2        Ga                                                  CH.sub.2 CF.sub.3         Ga                                                  CH.sub.2 CH.sub.2 Cl      Ga                                                  CH.sub.2 CH.sub.2 Br      Ga                                                  CH.sub.2 CH.sub.2 CF.sub.3                                                                              Ga                                                  CH.sub.2 CF.sub.2 CF.sub.3                                                                              Ga                                                  CH.sub.2 CHCHCl           Ga                                                  CH.sub.2 CHCHBr           Ga                                                  CH.sub.2 CHCF.sub.2       Ga                                                  CH.sub.2 CHCHCF.sub.3     Ga                                                  CH.sub.2 CCI              Gb                                                  CH.sub.2 CCCF.sub.3       Gb                                                  CH.sub.2 CN               Ga                                                  CH.sub.2 CH.sub.2 CN      Ga                                                  CHMeCN                    Ga                                                  CH.sub.2 CHCHCN           Ga                                                  CH(CN)CCH                 Gb                                                  CH.sub.2 NO.sub.2         Ga                                                  CH.sub.2 CH.sub.2 NO.sub.2                                                                              Ga                                                  CH.sub.2 CHCHNO.sub.2     Gb                                                  CH.sub.2 CH(NO.sub.2)CHCH.sub.2                                                                         Gc                                                  CH.sub.2 CH(NO.sub.2)C CH Gc                                                  CH.sub.2 CO.sub.2 Me      Gb                                                  CH.sub.2 CO.sub.2 Et      Gb                                                  CH.sub.2 CO.sub.2 Pr-n    Gb                                                  CHMeCO.sub.2 Me           Gb                                                  CHMeCO.sub.2 Et           Gb                                                  CH.sub.2 CH.sub.2 CO.sub.2 Me                                                                           Ga                                                  CH.sub.2 CH.sub.2 CO.sub.2 Et                                                                           Ga                                                  CH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 Me                                                                  Gb                                                  CH.sub.2 CHCHCO.sub.2 Me  Ga                                                  CH.sub.2 CHCHCO.sub.2 Et  Ga                                                  CHMeCHCHCO.sub.2 Me       Ga                                                  CHMeCHCHCO.sub.2 Et       Ga                                                  CH.sub.2 CCCO.sub.2 Me    Ga                                                  CH.sub.2 CCCO.sub.2 Et    Ga                                                  CH.sub.2 COMe             Ga                                                  CH.sub.2 COEt             Ga                                                  CH.sub.2 COPr-n           Gb                                                  CH.sub.2 CH.sub.2 COMe    Ga                                                  CH.sub.2 CH.sub.2 COEt    Ga                                                  CH.sub.2 COCF.sub.3       Ga                                                  CH.sub.2 CH.sub.2 COCF.sub.3                                                                            Ga                                                  CH.sub.2 COCH.sub.2 CF.sub.3                                                                            Gb                                                  CH.sub.2 COCH.sub.2 F     Gb                                                  CH.sub.2 COCHCH.sub.2     Ga                                                  CH.sub.2 COCHCHMe         Ga                                                  CH.sub.2 COCH.sub.2 CHCH.sub.2                                                                          Gb                                                  CH.sub.2 CH.sub.2 COCHCH.sub.2                                                                          Gb                                                  CH.sub.2 CH.sub. 2 COCHCHMe                                                                             Gb                                                  CH.sub.2 COCCH            Ga                                                  CH.sub.2 COCCMe           Ga                                                  CH.sub.2 COCH.sub.2 OMe   Ga                                                  CH.sub.2 COCH.sub.2 OEt   Ga                                                  CH.sub.2 COCH.sub.2 CH.sub.2 OMe                                                                        Ga                                                  CH.sub.2 COCH.sub.2 CH.sub.2 OEt                                                                        Ga                                                  CH.sub.2 COCH.sub.2 SMe   Ga                                                  CH.sub.2 COCH.sub.2 SEt   Ga                                                  CH.sub.2 COCH.sub.2 CH.sub.2 SMe                                                                        Ga                                                  CH.sub.2 COCH.sub.2 CH.sub.2 SEt                                                                        Ga                                                  CH.sub.2 COCH.sub.2 SOMe  Gb                                                  CH.sub.2 COCH.sub.2 CH.sub.2 SOMe                                                                       Gb                                                  CH.sub.2 COCH.sub.2 SO.sub.2 Me                                                                         Ga                                                  CH.sub.2 COCH.sub.2 SO.sub.2 Et                                                                         Ga                                                  CH.sub.2 COCH.sub.2 CH.sub.2 SO.sub.2 Me                                                                Ga                                                  CH.sub.2 COCH.sub.2 CH.sub.2 SO.sub.2 Et                                                                Ga                                                  CH.sub.2 CHCHCOMe         Ga                                                  CH.sub.2 CHCHCOEt         Ga                                                  CHMeCHCHCOMe              Ga                                                  CHMeCHCHCOEt              Ga                                                  CH.sub.2 CCCOMe           Ga                                                  CH.sub.2 CCCOEt           Ga                                                  CH.sub.2 SO.sub.2 NHMe    Ga                                                  CH.sub.2 SO.sub.2 NHEt    Ga                                                  CH.sub.2 CH.sub.2 SO.sub.2 NHMe                                                                         Ga                                                  CH.sub.2 CH.sub.2 SO.sub.2 NHEt                                                                         Ga                                                  CH.sub.2 SO.sub.2 NHOMe   Ga                                                  CH.sub.2 SO.sub.2 NHOEt   Ga                                                  CH.sub.2 CH.sub.2 SO.sub.2 NHOMe                                                                        Ga                                                  CH.sub.2 CH.sub.2 SO.sub.2 NHOEt                                                                        Ga                                                  CH.sub.2 SO.sub.2 NMe.sub.2                                                                             Ga                                                  CH.sub.2 SO.sub.2 NMeEt   Ga                                                  CH.sub.2 SO.sub.2 NEt.sub.2                                                                             Ga                                                  CH.sub.2 CH.sub.2 SO.sub.2 NMe.sub.2                                                                    Ga                                                  CH.sub.2 CH.sub.2 SO.sub.2 NMeEt                                                                        Ga                                                  CH.sub.2 CH.sub.2 SO.sub.2 NEt.sub.2                                                                    Ga                                                  CH.sub.2 SO.sub.2 N(OMe)Me                                                                              Ga                                                  CH.sub.2 SO.sub.2 N(OMe)Et                                                                              Ga                                                  CH.sub.2 SO.sub.2 N(OEt)Me                                                                              Ga                                                  CH.sub.2 CH.sub.2 SO.sub.2 N(OMe)Me                                                                     Ga                                                  CH.sub.2 CH.sub.2 SO.sub.2 N(OMe)Et                                                                     Ga                                                  CH.sub.2 CH.sub.2 SO.sub.2 N(OEt)Me                                                                     Ga                                                  CH.sub.2 CONHMe           Ga                                                  CH.sub.2 CONHEt           Ga                                                  CH.sub.2 CONHPr-n         Gb                                                  CH.sub.2 CH.sub.2 CONHMe  Ga                                                  CH.sub.2 CH.sub.2 CONHEt  Ga                                                  CH.sub.2 CH.sub.2 CONHPr-n                                                                              Gb                                                  CH.sub.2 CONMe.sub.2      Ga                                                  CH.sub.2 CONMeEt          Ga                                                  CH.sub.2 CONEt.sub.2      Ga                                                  CH.sub.2 CONHOMe          Ga                                                  CH.sub.2 CONHOEt          Ga                                                  CH.sub.2 CONHOPr-n        Gb                                                  CH.sub.2 CON(OMe)Me       Ga                                                  CH.sub.2 CON(OMe)Et       Ga                                                  CH.sub.2 CON(OEt)Me       Ga                                                  CH.sub.2 CON(OEt)Et       Ga                                                  CH.sub.2 NHMe             Ga                                                  CH.sub.2 NHEt             Ga                                                  CH.sub.2 NHPr-n           Gb                                                  CH.sub.2 CH.sub.2 NHMe    Ga                                                  CH.sub.2 CH.sub.2 NHEt    Ga                                                  CH.sub.2 CH.sub.2 NHPr-n  Gb                                                  CH.sub.2 NHOMe            Ga                                                  CH.sub.2 NHOEt            Ga                                                  CH.sub.2 CH.sub.2 NHOMe   Ga                                                  CH.sub.2 CH.sub.2 NHOEt   Ga                                                  CH.sub.2 NMe.sub.2        Ga                                                  CH.sub.2 NMeEt            Ga                                                  CH.sub.2 CH.sub.2 NMe.sub.2                                                                             Ga                                                  CH.sub.2 CH.sub.2 NMeEt   Ga                                                  CH.sub.2 N(OMe)Me         Ga                                                  CH.sub.2 N(OMe)Et         Ga                                                  CH.sub.2 N(OEt)Me         Ga                                                  CH.sub.2 CH.sub.2 N(OMe)Me                                                                              Ga                                                  CH.sub.2 CH.sub.2 N(OMe)Et                                                                              Ga                                                  CH.sub.2 CH.sub.2 N(OEt)Me                                                                              Ga                                                  CH.sub.2 NMeCOMe          Ga                                                  CH.sub.2 NEtCOMe          Ga                                                  CH.sub.2 NMeCOEt          Ga                                                  CH.sub.2 CH.sub.2 NMeCOMe Ga                                                  CH.sub.2 CH.sub.2 NEtCOMe Ga                                                  CH.sub.2 CH.sub.2 NMeCOEt Ga                                                  CH.sub.2 N(OMe)COMe       Ga                                                  CH.sub.2 N(OEt)COMe       Ga                                                  CH.sub.2 N(OMe)COEt       Ga                                                  CH.sub.2 CH.sub.2 N(OMe)COMe                                                                            Ga                                                  CH.sub.2 CH.sub.2 N(OEt)COMe                                                                            Ga                                                  CH.sub.2 CH.sub.2 N(OMe)COEt                                                                            Ga                                                  CH.sub.2 NMeSO.sub.2 Me   Ga                                                  CH.sub.2 NEtSO.sub.2 Me   Ga                                                  CH.sub.2 NMeSO.sub.2 Et   Ga                                                  CH.sub.2 CH.sub.2 NMeSO.sub.2 Me                                                                        Ga                                                  CH.sub.2 CH.sub.2 NEtSO.sub.2 Me                                                                        Ga                                                  CH.sub.2 CH.sub.2 NMeSO.sub.2 Et                                                                        Ga                                                  CH.sub.2 N(OMe)SO.sub.2 Me                                                                              Ga                                                  CH.sub.2 N(OEt)SO.sub.2 Me                                                                              Ga                                                  CH.sub.2 N(OMe)SO.sub.2 Et                                                                              Ga                                                  CH.sub.2 CH.sub.2 N(OMe)SO.sub.2 Me                                                                     Ga                                                  CH.sub.2 CH.sub.2 N(OEt)SO.sub.2 Me                                                                     Ga                                                  CH.sub.2 CH.sub.2 N(OMe)SO.sub.2 Et                                                                     Ga                                                  CH.sub.2 Ph               Gb                                                  CH.sub.2 CH.sub.2 Ph      Gb                                                  CH.sub.2 CH.sub.2 CH.sub.2 Ph                                                                           Gb                                                  CHMePh                    Gb                                                  CH.sub.2 CHCHPh           Ga                                                  CHMeCHCHPh                Ga                                                  CH.sub.2 CCPh             Ga                                                  CHMeCCPh                  Ga                                                  CH.sub.2 CH.sub.2 OPh     Ga                                                  CH.sub.2 OPh              Ga                                                  CH.sub.2 CH.sub.2 SPh     Ga                                                  CH.sub.2 SPh              Ga                                                  CH.sub.2 CH.sub.2 SOPh    Gb                                                  CH.sub.2 CH.sub.2 SO.sub.2 Ph                                                                           Ga                                                  CH.sub.2 OCH.sub.2 Ph     Ga                                                  CH.sub.2 CH.sub.2 OCH.sub.2 Ph                                                                          Ga                                                  CH.sub.2 SCH.sub.2 Ph     Ga                                                  CH.sub.2 CH.sub.2 SCH.sub.2 Ph                                                                          Ga                                                  CH.sub.2 SOCH.sub.2 Ph    Gb                                                  CH.sub.2 CH.sub.2 SOCH.sub.2 Ph                                                                         Gb                                                  CH.sub.2 SO.sub.2 CH.sub.2 Ph                                                                           Ga                                                  CH.sub.2 CH.sub.2 SO.sub.2 CH.sub.2 Ph                                                                  Ga                                                  CH.sub.2 COPh             Ga                                                  CH.sub.2 CH.sub.2 COPh    Ga                                                  CHMeCOPh                  Ga                                                  CH.sub.2 COCH.sub.2 Ph    Gb                                                  CHMeCOCH.sub.2 Ph         Gb                                                  CH.sub.2 CH.sub.2 CH.sub.2 F                                                                            Ga                                                  CH.sub.2 CH.sub.2 CH.sub.2 Cl                                                                           Ga                                                  CH.sub.2 C(Cl)CH.sub.2    Ga                                                  CH.sub.2 C(Br)CH.sub.2    Ga                                                  Ph                        Ga                                                  CH.sub.2 SOPh             Ga                                                  CH.sub.2 SO.sub.2 Ph      Ga                                                  CH.sub.2 Ph-4-OMe         Gb                                                  CH.sub.2 Ph-4-Cl          Gb                                                  CH.sub.2 C(Cl)CHCl        Ga                                                  CH.sub.2 C(F)CHCl         Ga                                                  CH.sub.2 CHCHF            Ga                                                  CH.sub.2 C(Cl)CHMe        Ga                                                  CH.sub.2 CHC(Cl)Me        Ga                                                  CH.sub.2 CFCF.sub.2       Ga                                                  CH.sub.2 CHCHCH.sub.2 F   Ga                                                  CH.sub.2 C(Br)CHMe        Ga                                                  CH.sub.2 C(Cl)CHF         Ga                                                  CH.sub.2 C(Br)CHF         Ga                                                  CH.sub.2 C(Cl)C(Cl)Me     Ga                                                  CH.sub.2 C(Br)CHBr        Ga                                                  CH.sub.2 C(Br)C(Br)Me     Ga                                                  CH.sub.2 CHC(F)CF.sub.3   Ga                                                  CH.sub.2 CHCCl.sub.2      Ga                                                  CH.sub.2 C(F)CH.sub.2     Ga                                                  CH.sub.2 CHC(F)Cl         Ga                                                  CH.sub.2 C(Cl)C(F)Cl      Ga                                                  CH.sub.2 C(F)CCl.sub.2    Ga                                                  CH.sub.2 CClCF.sub.2      Ga                                                  CH.sub.2 C(CF.sub.3)CH.sub.2                                                                            Ga                                                  CH.sub.2 NHSO.sub.2 Me    Gb                                                  CH.sub.2 CH.sub.2 NHSO.sub.2 Me                                                                         Gb                                                  CH.sub.2 NHCOMe           Gb                                                  CH.sub.2 CH.sub.2 NHCOMe  Gb                                                  ______________________________________                                         R.sup.m represents R.sup.a1, R.sup.b1, R.sup.d1, R.sup.e1 or R.sup.f1.   

                  TABLE 1B                                                        ______________________________________                                         ##STR55##                                                                    Q:                                                                                 ##STR56##                                                                     ##STR57##                                                                     ##STR58##                                                                     ##STR59##                                                                     ##STR60##                                                                     ##STR61##                                                                     ##STR62##                                                                     ##STR63##                                                                     ##STR64##                                                                     ##STR65##                                                                     ##STR66##                                                                     ##STR67##                                                                     ##STR68##                                                                     ##STR69##                                                                     ##STR70##                                                                     ##STR71##                                                                     ##STR72##                                                                     ##STR73##                                                                     ##STR74##                                                                     ##STR75##                                                                     ##STR76##                                                                     ##STR77##                                                                     ##STR78##                                                                     ##STR79##                                                                     ##STR80##                                                                     ##STR81##                                                                     ##STR82##                                                                     ##STR83##                                                                     ##STR84##                                                                     ##STR85##                                                                     ##STR86##                                                                     ##STR87##                                                                     ##STR88##                                                                     ##STR89##                                                                     ##STR90##                                                                     ##STR91##                                                                     ##STR92##                                                                     ##STR93##                                                                     ##STR94##                                                                     ##STR95##                                                                     ##STR96##                                                                     ##STR97##                                                                     ##STR98##                                                                     ##STR99##                                                                     ##STR100##                                                                    ##STR101##                                                                    ##STR102##                                                                    ##STR103##                                                                    ##STR104##                                                                    ##STR105##                                                                    ##STR106##                                                                    ##STR107##                                                                    ##STR108##                                                                    ##STR109##                                                                    ##STR110##                                                                    ##STR111##                                                                    ##STR112##                                                                    ##STR113##                                                                    ##STR114##                                                                    ##STR115##                                                                    ##STR116##                                                                    ##STR117##                                                                    ##STR118##                                                                    ##STR119##                                                                    ##STR120##                                                                    ##STR121##                                                                    ##STR122##                                                                    ##STR123##                                                                    ##STR124##                                                                    ##STR125##                                                                    ##STR126##                                                                    ##STR127##                                                                    ##STR128##                                                                    ##STR129##                                                                    ##STR130##                                                                    ##STR131##                                                                    ##STR132##                                                                    ##STR133##                                                                    ##STR134##                                                                    ##STR135##                                                                    ##STR136##                                                                    ##STR137##                                                                    ##STR138##                                                                    ##STR139##                                                                    ##STR140##                                                                    ##STR141##                                                                    ##STR142##                                                                    ##STR143##                                                                    ##STR144##                                                                    ##STR145##                                                                    ##STR146##                                                                    ##STR147##                                                                    ##STR148##                                                                    ##STR149##                                                                    ##STR150##                                                                    ##STR151##                                                                    ##STR152##                                                                    ##STR153##                                                                    ##STR154##                                                                    ##STR155##                                                                    ##STR156##                                                                    ##STR157##                                                                    ##STR158##                                                                    ##STR159##                                                                    ##STR160##                                                                    ##STR161##                                                                    ##STR162##                                                                    ##STR163##                                                                    ##STR164##                                                                    ##STR165##                                                                    ##STR166##                                                                    ##STR167##                                                                    ##STR168##                                                                    ##STR169##                                                                    ##STR170##                                                                    ##STR171##                                                                    ##STR172##                                                                    ##STR173##                                                                    ##STR174##                                                                    ##STR175##                                                                    ##STR176##                                                                    ##STR177##                                                                    ##STR178##                                                                    ##STR179##                                                                    ##STR180##                                                                    ##STR181##                                                                    ##STR182##                                                                    ##STR183##                                                                    ##STR184##                                                                    ##STR185##                                                                    ##STR186##                                                                    ##STR187##                                                                    ##STR188##                                                                    ##STR189##                                                                    ##STR190##                                                                    ##STR191##                                                                    ##STR192##                                                                    ##STR193##                                                                    ##STR194##                                                                    ##STR195##                                                                    ##STR196##                                                                    ##STR197##                                                                    ##STR198##                                                                    ##STR199##                                                                    ##STR200##                                                                    ##STR201##                                                               ______________________________________                                        R.sup.m            Gn                                                         ______________________________________                                        Me                 Ga                                                         Et                 Ga                                                         Pr-n               Ga                                                         Pr-iso             Ga                                                         Bu-n               Ga                                                         Bu-iso             Gb                                                         Pen-n              Gb                                                         Hex-n              Gb                                                         CH.sub.2 Pr-cyc    Ga                                                         CH.sub.2 CH.sub.2 Pr-cyc                                                                         Ga                                                         CH.sub.2 CHCH.sub.2                                                                              Ga                                                         CH.sub.2 CHCHMe    Ga                                                         CH.sub.2 CCH       Ga                                                         CH.sub.2 CCMe      Ga                                                         CH.sub.2 OMe       Ga                                                         CH.sub.2 OEt       Ga                                                         CH.sub.2 CH.sub.2 OMe                                                                            Ga                                                         CH.sub.2 CH.sub.2 OEt                                                                            Ga                                                         CH.sub.2 OCH.sub.2 CHCH.sub.2                                                                    Ga                                                         CH.sub.2 CH.sub.2 OCH.sub.2 CHCH.sub.2                                                           Ga                                                         CH.sub.2 OCH.sub.2 CCH                                                                           Ga                                                         CH.sub.2 CH.sub.2 OCH.sub.2 CCH                                                                  Ga                                                         CH.sub.2 OCH.sub.2 CF.sub.3                                                                      Ga                                                         CH.sub.2 CH.sub.2 OCH.sub.2 CF.sub.3                                                             Ga                                                         CH.sub.2 SMe       Ga                                                         CH.sub.2 SEt       Ga                                                         CH.sub.2 CH.sub.2 SMe                                                                            Ga                                                         CH.sub.2 CH.sub.2 SEt                                                                            Ga                                                         CH.sub.2 SO.sub.2 Me                                                                             Ga                                                         CH.sub.2 SO.sub.2 Et                                                                             Ga                                                         CH.sub.2 CH.sub.2 SO.sub.2 Me                                                                    Ga                                                         CH.sub.2 CH.sub.2 SO.sub.2 Et                                                                    Ga                                                         CH.sub.2 CH.sub.2 F                                                                              Ga                                                         CH.sub.2 CF.sub.3  Ga                                                         CH.sub.2 CN        Ga                                                         CH.sub.2 CH.sub.2 CN                                                                             Ga                                                         CHMeCN             Ga                                                         CH.sub.2 CHCHCN    Ga                                                         CH.sub.2 NO.sub.2  Ga                                                         CH.sub.2 CH.sub.2 NO.sub.2                                                                       Ga                                                         CH.sub.2 CO.sub.2 Me                                                                             Gb                                                         CH.sub.2 CO.sub.2 Et                                                                             Gb                                                         CHMeCO.sub.2 Me    Gb                                                         CHMeCO.sub.2 Et    Gb                                                         CH.sub.2 CH.sub.2 CO.sub.2 Me                                                                    Ga                                                         CH.sub.2 CH.sub.2 CO.sub.2 Et                                                                    Ga                                                         CH.sub.2 CHCHCO.sub.2 Me                                                                         Ga                                                         CH.sub.2 CHCHCO.sub.2 Et                                                                         Ga                                                         CHMeCHCHCO.sub.2 Me                                                                              Ga                                                         CH.sub.2 COMe      Ga                                                         CH.sub.2 COEt      Ga                                                         CH.sub.2 COPr-n    Gb                                                         CH.sub.2 COCF.sub.3                                                                              Ga                                                         CH.sub.2 COCHCH.sub.2                                                                            Ga                                                         CH.sub.2 COCHCHMe  Ga                                                         CH.sub.2 COCH.sub.2 OMe                                                                          Ga                                                         CH.sub.2 COCH.sub.2 OEt                                                                          Ga                                                         CH.sub.2 COCH.sub.2 CH.sub.2 OMe                                                                 Ga                                                         CH.sub.2 COCH.sub.2 CH.sub.2 OEt                                                                 Ga                                                         CH.sub.2 COCH.sub.2 SMe                                                                          Ga                                                         CH.sub.2 COCH.sub.2 CH.sub.2 SMe                                                                 Ga                                                         CH.sub.2 COCH.sub.2 SO.sub.2 Me                                                                  Ga                                                         CH.sub.2 COCH.sub.2 CH.sub.2 SO.sub.2 Me                                                         Ga                                                         CH.sub.2 CHCHCOMe  Ga                                                         CHMeCHCHCOMe       Ga                                                         CH.sub.2 SO.sub.2 NHMe                                                                           Gb                                                         CH.sub.2 CH.sub.2 SO.sub.2 NHMe                                                                  Gb                                                         CH.sub.2 SO.sub.2 NHOMe                                                                          Gb                                                         CH.sub.2 CH.sub.2 SO.sub.2 NHOMe                                                                 Gb                                                         CH.sub.2 SO.sub.2 NMe.sub.2                                                                      Ga                                                         CH.sub.2 CH.sub.2 SO.sub.2 NMe.sub.2                                                             Ga                                                         CH.sub.2 SO.sub.2 N(OMe)Me                                                                       Ga                                                         CH.sub.2 CH.sub.2 SO.sub.2 N(OMe)Me                                                              Ga                                                         CH.sub.2 CONHMe    Gb                                                         CH.sub.2 CH.sub.2 CONHMe                                                                         Gb                                                         CH.sub.2 CONMe.sub.2                                                                             Ga                                                         CH.sub.2 CH.sub.2 CONMe.sub.2                                                                    Ga                                                         CH.sub.2 CONHOMe   Gb                                                         CH.sub.2 CH.sub.2 CONHMe                                                                         Gb                                                         CH.sub.2 CON(OMe)Me                                                                              Ga                                                         CH.sub.2 CH.sub.2 CON(OMe)Me                                                                     Ga                                                         CH.sub.2 NHMe      Gb                                                         CH.sub.2 CH.sub.2 NHMe                                                                           Gb                                                         CH.sub.2 CHOMe     Gb                                                         CH.sub.2 CH.sub.2 NHOMe                                                                          Gb                                                         CH.sub.2 NMe.sub.2 Ga                                                         CH.sub.2 CH.sub.2 NMe.sub.2                                                                      Ga                                                         CH.sub.2 N(OMe)Me  Ga                                                         CH.sub.2 CH.sub.2 N(OMe)Me                                                                       Ga                                                         CH.sub.2 NMeCOMe   Ga                                                         CH.sub.2 CH.sub.2 NMeCOMe                                                                        Ga                                                         CH.sub.2 N(OMe)COMe                                                                              Ga                                                         CH.sub.2 CH.sub.2 N(OMe)COMe                                                                     Ga                                                         CH.sub.2 NMeSO.sub.2 Me                                                                          Ga                                                         CH.sub.2 CH.sub.2 NMeSO.sub.2 Me                                                                 Ga                                                         CH.sub.2 N(OMe)SO.sub.2 Me Ga                                                 CH.sub.2 CH.sub.2 N(OMe)SO.sub.2 Me                                                              Ga                                                         CH.sub.2 Ph        Gb                                                         CH.sub.2 CH.sub.2 Ph                                                                             Gb                                                         CH.sub.2 CH.sub.2 CH.sub.2 Ph                                                                    Gb                                                         CHMePh             Gb                                                         CH.sub.2 CHCHPh    Gb                                                         CHMeCHCHPh         Gb                                                         CH.sub.2 CH.sub.2 OPh                                                                            Gb                                                         CH.sub.2 OPh       GB                                                         CH.sub.2 CH.sub.2 OPh                                                                            Gb                                                         CH.sub.2 SPh       Gb                                                         CH.sub.2 CH.sub.2 SO.sub.2 Ph                                                                    Gb                                                         CH.sub.2 COPh      Gb                                                         CH.sub.2 CH.sub.2 COPh                                                                           Gb                                                         CH.sub.2 COCH.sub.2 Ph                                                                           Gb                                                         CH.sub.2 CH.sub.2 COCH.sub.2 Ph                                                                  Gb                                                         Ph                 Gb                                                         ______________________________________                                    

                  TABLE 1C                                                        ______________________________________                                         ##STR202##                                                                   Q:                                                                                 ##STR203##                                                                    ##STR204##                                                                    ##STR205##                                                                    ##STR206##                                                                    ##STR207##                                                                    ##STR208##                                                                    ##STR209##                                                                    ##STR210##                                                                    ##STR211##                                                                    ##STR212##                                                                    ##STR213##                                                                    ##STR214##                                                                    ##STR215##                                                                    ##STR216##                                                                    ##STR217##                                                                    ##STR218##                                                                    ##STR219##                                                                    ##STR220##                                                                    ##STR221##                                                                    ##STR222##                                                                    ##STR223##                                                                    ##STR224##                                                                    ##STR225##                                                                    ##STR226##                                                                    ##STR227##                                                                    ##STR228##                                                                    ##STR229##                                                                    ##STR230##                                                                    ##STR231##                                                                    ##STR232##                                                                    ##STR233##                                                                    ##STR234##                                                                    ##STR235##                                                                    ##STR236##                                                                    ##STR237##                                                                    ##STR238##                                                                    ##STR239##                                                                    ##STR240##                                                                    ##STR241##                                                                    ##STR242##                                                                    ##STR243##                                                                    ##STR244##                                                                    ##STR245##                                                                    ##STR246##                                                                    ##STR247##                                                                    ##STR248##                                                                    ##STR249##                                                                    ##STR250##                                                                    ##STR251##                                                                    ##STR252##                                                                    ##STR253##                                                                    ##STR254##                                                                    ##STR255##                                                                    ##STR256##                                                                    ##STR257##                                                                    ##STR258##                                                                    ##STR259##                                                                    ##STR260##                                                                    ##STR261##                                                                    ##STR262##                                                                    ##STR263##                                                                    ##STR264##                                                                    ##STR265##                                                                    ##STR266##                                                                    ##STR267##                                                                    ##STR268##                                                                    ##STR269##                                                                    ##STR270##                                                                    ##STR271##                                                                    ##STR272##                                                                    ##STR273##                                                                    ##STR274##                                                                    ##STR275##                                                                    ##STR276##                                                                    ##STR277##                                                                    ##STR278##                                                                    ##STR279##                                                                    ##STR280##                                                                    ##STR281##                                                                    ##STR282##                                                                    ##STR283##                                                                    ##STR284##                                                                    ##STR285##                                                                    ##STR286##                                                                    ##STR287##                                                                    ##STR288##                                                                    ##STR289##                                                                    ##STR290##                                                                    ##STR291##                                                                    ##STR292##                                                                    ##STR293##                                                                    ##STR294##                                                                    ##STR295##                                                                    ##STR296##                                                                    ##STR297##                                                                    ##STR298##                                                                    ##STR299##                                                                    ##STR300##                                                                    ##STR301##                                                                    ##STR302##                                                                    ##STR303##                                                                    ##STR304##                                                                    ##STR305##                                                                    ##STR306##                                                                    ##STR307##                                                                    ##STR308##                                                                    ##STR309##                                                                    ##STR310##                                                                    ##STR311##                                                                    ##STR312##                                                                    ##STR313##                                                                    ##STR314##                                                                    ##STR315##                                                                    ##STR316##                                                                    ##STR317##                                                                    ##STR318##                                                                    ##STR319##                                                                    ##STR320##                                                                    ##STR321##                                                                    ##STR322##                                                                    ##STR323##                                                                    ##STR324##                                                                    ##STR325##                                                                    ##STR326##                                                                    ##STR327##                                                                    ##STR328##                                                                    ##STR329##                                                                    ##STR330##                                                                    ##STR331##                                                                    ##STR332##                                                                    ##STR333##                                                                    ##STR334##                                                                    ##STR335##                                                                    ##STR336##                                                                    ##STR337##                                                                    ##STR338##                                                                    ##STR339##                                                                    ##STR340##                                                                    ##STR341##                                                                    ##STR342##                                                                    ##STR343##                                                                    ##STR344##                                                                    ##STR345##                                                                    ##STR346##                                                                    ##STR347##                                                                    ##STR348##                                                               ______________________________________                                        R.sup.m            Gn                                                         ______________________________________                                        Me                 Ga                                                         Et                 Ga                                                         Pr-n               Ga                                                         Pr-iso             Gb                                                         Bu-n               Ga                                                         Bu-iso             Ga                                                         Pen-n              Gb                                                         CH.sub.2 Pr-cyc    Ga                                                         CH.sub.2 CH.sub.2 Pr-cyc                                                                         Gb                                                         CH.sub.2 CHCH.sub.2                                                                              Ga                                                         CH.sub.2 CHCHMe    Ga                                                         CH.sub.2 CCH       Ga                                                         CH.sub.2 CCMe      Ga                                                         CH.sub.2 CH.sub.2 OMe                                                                            Ga                                                         CH.sub.2 OMe       Ga                                                         CH.sub.2 CH.sub.2 SMe                                                                            Ga                                                         CH.sub.2 SMe       Ga                                                         CH.sub.2 SO.sub.2 Me                                                                             Ga                                                         CH.sub.2 CH.sub.2 SO.sub.2 Me                                                                    Ga                                                         CH.sub.2 CF.sub.3  Ga                                                         CH.sub.2 CN        Ga                                                         CH.sub.2 CH.sub.2 CN                                                                             Ga                                                         CH.sub.2 NO.sub.2  Ga                                                         CH.sub.2 CH.sub.2 NO.sub.2                                                                       Ga                                                         CH.sub.2 COMe      Ga                                                         CH.sub.2 COEt      Ga                                                         CH.sub.2 COCHCH.sub.2                                                                            Ga                                                         CH.sub.2 CHCHCOMe  Ga                                                         CH.sub.2 CONMe.sub.2                                                                             Ga                                                         ______________________________________                                         R.sup.m represents R.sup.a1, R.sup.b1, R.sup.d1, R.sup.e1, or R.sup.f1.  

                  TABLE 2A                                                        ______________________________________                                         ##STR349##                                                                    ##STR350##                                                                    ##STR351##                                                                    ##STR352##                                                                   R.sup.c1                  Gn                                                  ______________________________________                                        Me                       Ga                                                   Et                       Ga                                                   Pr-n                     Ga                                                   Pr-iso                   Ga                                                   Bu-n                     Ga                                                   Bu-iso                   Ga                                                   Bu-sec                   Ga                                                   Bu-tert                  Gb                                                   Pen-n                    Ga                                                   Hex-n                    Gb                                                   Hep-n                    Gb                                                   Pr-cyc                   Ga                                                   Hex-cyc                  Ga                                                   CH.sub.2 Pr-cyc          Ga                                                   CH.sub.2 CH.sub.2 Pr-cyc Ga                                                   CH.sub.2 Bu-cyc          Gb                                                   CH.sub.2 Pen-cyc         Gc                                                   Hexen-cyc                Gb                                                   CH.sub.2 Penten-cyc      Gb                                                   CH.sub.2 CHCH.sub.2      Ga                                                   CH.sub.2 CHCHMe          Ga                                                   CH.sub.2 CHCHEt          Ga                                                   CH.sub.2 CHCMe.sub.2     Ga                                                   CH.sub.2 CMeCH.sub.2     Ga                                                   CH.sub.2 CMeCHCHMe       Ga                                                   CH.sub.2 CH.sub.2 CHCH.sub.2                                                                           Ga                                                   CH.sub.2 CH.sub.2 CHCHMe Ga                                                   CH.sub.2 CCH             Ga                                                   CH.sub.2 CCMe            Ga                                                   CH.sub.2 CCEt            Ga                                                   CH.sub.2 CH.sub.2 CCH    Ga                                                   CH.sub.2 CH.sub.2 CCMe   Ga                                                   CHMeCCH                  Ga                                                   CHMeC CMe                Ga                                                   CH.sub.2 OMe             Ga                                                   CH.sub.2 OEt             Ga                                                   CH.sub.2 OPr-n           Gb                                                   CH.sub.2 CH.sub.2 OMe    Ga                                                   CH.sub.2 CH.sub.2 OEt    Ga                                                   CH.sub.2 CH.sub.2 OPr-n  Gb                                                   CH.sub.2 CHMeOMe         Ga                                                   CH.sub.2 CH.sub.2 CH.sub.2 OMe                                                                         Ga                                                   CH.sub.2 CH.sub.2 CH.sub.2 OEt                                                                         Ga                                                   CH.sub.2 OCH.sub.2 CHCH.sub.2                                                                          Ga                                                   CH.sub.2 OCH.sub.2 CHCHMe                                                                              Ga                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CHCH.sub.2                                                                 Ga                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CHCHMe                                                                     Ga                                                   CH.sub.2 OCH.sub.2 CCH   Ga                                                   CH.sub.2 OCH.sub.2 CCMe  Ga                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CCH                                                                        Ga                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CCMe                                                                       Ga                                                   CH.sub.2 OCHF.sub.2      Ga                                                   CH.sub.2 OCF.sub.3       Ga                                                   CH.sub.2 CH.sub.2 OCHF.sub.2                                                                           Ga                                                   CH.sub.2 CH.sub.2 OCF.sub.3                                                                            Ga                                                   CH.sub.2 OCH.sub.2 CF.sub.3                                                                            Ga                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CF.sub.3                                                                   Ga                                                   CH.sub.2 OCH.sub.2 CH.sub.2 F                                                                          Ga                                                   CH.sub.2 OCH.sub.2 CH.sub.2 Cl                                                                         Ga                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 F                                                                 Ga                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 Cl                                                                Ga                                                   CH.sub.2 OCH.sub.2 CHCHCl                                                                              Gb                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CHCHCl                                                                     Gb                                                   CH.sub.2 OCH.sub.2 CHCHBr                                                                              Gb                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CHCHBr                                                                     Gb                                                   CH.sub.2 OCH.sub.2 CHCF.sub.2                                                                          Gb                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CHCF.sub.2                                                                 Gb                                                   CH.sub.2 OCH.sub.2 CHCHCF.sub.3                                                                        Gb                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CHCHCF.sub.3                                                               Gb                                                   CH.sub.2 OCH.sub.2 CCI   Gb                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CCI                                                                        Gb                                                   CH.sub.2 OCH.sub.2 CCCF.sub.3                                                                          Gb                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CCCF.sub.3                                                                 Gb                                                   CH.sub.2 SMe             Ga                                                   CH.sub.2 SEt             Ga                                                   CH.sub.2 SPr-n           Gb                                                   CH.sub.2 CH.sub.2 SMe    Ga                                                   CH.sub. 2 CH.sub.2 SEt   Ga                                                   CH.sub.2 CH.sub.2 SPr-n  Gb                                                   CH.sub.2 SOMe            Gb                                                   CH.sub.2 SOEt            Gb                                                   CH.sub.2 CH.sub.2 SOMe   Gb                                                   CH.sub.2 CH.sub.2 SOEt   Gb                                                   CH.sub.2 SO.sub.2 Me     Ga                                                   CH.sub.2 SO.sub.2 Et     Ga                                                   CH.sub.2 SO.sub.2 Pr-n   Gb                                                   CH.sub.2 CH.sub.2 SO.sub.2 Me                                                                          Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 Et                                                                          Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 Pr-n                                                                        Gb                                                   CH.sub.2 CH.sub.2 F      Ga                                                   CH.sub.2 CHF.sub.2       Ga                                                   CH.sub.2 CF.sub.3        Ga                                                   CH.sub.2 CH.sub.2 Cl     Ga                                                   CH.sub.2 CH.sub.2 Br     Ga                                                   CH.sub.2 CH.sub.2 CF.sub.3                                                                             Ga                                                   CH.sub.2 CF.sub.2 CF.sub.3                                                                             Ga                                                   CH.sub.2 CHCHCl          Ga                                                   CH.sub.2 CHCHBr          Ga                                                   CH.sub.2 CHCF.sub.2      Ga                                                   CH.sub.2 CHCHCF.sub.3    Ga                                                   CH.sub.2 CCI             Gb                                                   CH.sub.2 CCCF.sub.3      Gb                                                   CH.sub.2 CN              Ga                                                   CH.sub.2 CH.sub.2 CN     Ga                                                   CHMeCN                   Ga                                                   CH.sub.2 CHCHCN          Ga                                                   CH(CN)CCH                Gb                                                   CH.sub.2 NO.sub.2        Ga                                                   CH.sub.2 CH.sub.2 NO.sub.2                                                                             Ga                                                   CH.sub.2 CHCHNO.sub.2    Gb                                                   CH.sub.2 CH(NO.sub.2)CHCH.sub.2                                                                        Gc                                                   CH.sub.2 CH(NO.sub.2)CCH Gc                                                   CH.sub.2 CO.sub.2 Me     Ga                                                   CH.sub.2 CO.sub.2 Et     Ga                                                   CH.sub.2 CO.sub.2 Pr-n   Gb                                                   CHMeCO.sub.2 Me          Ga                                                   CHMeCO.sub.2 Et          Ga                                                   CH.sub.2 CH.sub.2 CO.sub.2 Me                                                                          Ga                                                   CH.sub.2 CH.sub.2 CO.sub.2 Et                                                                          Ga                                                   CH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 Me                                                                 Gb                                                   CH.sub.2 CHCHCO.sub.2 Me Ga                                                   CH.sub.2 CHCHCO.sub.2 Et Ga                                                   CHMeCHCHCO.sub.2 Me      Ga                                                   CHMeCHCHCO.sub.2 Et      Ga                                                   CH.sub.2 CCCO.sub.2 Me   Ga                                                   CH.sub.2 CCCO.sub.2 Et   Ga                                                   CH.sub.2 COMe            Ga                                                   CH.sub.2 COEt            Ga                                                   CH.sub.2 COPr-n          Gb                                                   CH.sub.2 CH.sub.2 COMe   Ga                                                   CH.sub.2 CH.sub.2 COEt   Ga                                                   CH.sub.2 COCF.sub.3      Ga                                                   CH.sub.2 CH.sub.2 COCF.sub.3                                                                           Ga                                                   CH.sub.2 COCH.sub.2 CF.sub.3                                                                           Gb                                                   CH.sub.2 COCH.sub.2 F    Gb                                                   CH.sub.2 COCHCH.sub.2    Ga                                                   CH.sub.2 COCHCHMe        Ga                                                   CH.sub.2 COCH.sub.2 CHCH.sub.2                                                                         Gb                                                   CH.sub.2 CH.sub.2 COCHCH.sub.2                                                                         Gb                                                   CH.sub.2 CH.sub.2 COCHCHMe                                                                             Gb                                                   CH.sub.2 COCCH           Ga                                                   CH.sub.2 COCCMe          Ga                                                   CH.sub.2 COCH.sub.2 OMe  Ga                                                   CH.sub.2 COCH.sub.2 OEt  Ga                                                   CH.sub.2 COCH.sub.2 CH.sub.2 OMe                                                                       Ga                                                   CH.sub.2 COCH.sub.2 CH.sub.2 OEt                                                                       Ga                                                   CH.sub.2 COCH.sub.2 SMe  Ga                                                   CH.sub.2 COCH.sub.2 SEt  Ga                                                   CH.sub.2 COCH.sub.2 CH.sub.2 SMe                                                                       Ga                                                   CH.sub.2 COCH.sub.2 CH.sub.2 SEt                                                                       Ga                                                   CH.sub.2 COCH.sub.2 SOMe Gb                                                   CH.sub.2 COCH.sub.2 CH.sub.2 SOMe                                                                      Gb                                                   CH.sub.2 COCH.sub.2 SO.sub.2 Me                                                                        Ga                                                   CH.sub.2 COCH.sub.2 SO.sub.2 Et                                                                        Ga                                                   CH.sub.2 COCH.sub.2 CH.sub.2 SO.sub.2 Me                                                               Ga                                                   CH.sub.2 COCH.sub.2 CH.sub.2 SO.sub.2 Et                                                               Ga                                                   CH.sub.2 CHCHCOMe        Ga                                                   CH.sub.2 CHCHCOEt        Ga                                                   CHMeCHCHCOMe             Ga                                                   CHMeCHCHCOEt             Ga                                                   CH.sub.2 CCCOMe          Ga                                                   CH.sub.2 CCCOEt          Ga                                                   CH.sub.2 SO.sub.2 NHMe   Ga                                                   CH.sub.2 SO.sub.2 NHEt   Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 NHMe                                                                        Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 NHEt                                                                        Ga                                                   CH.sub.2 SO.sub.2 NHOMe  Ga                                                   CH.sub.2 SO.sub.2 NHOEt  Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 NHOMe                                                                       Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 NHOEt                                                                       Ga                                                   CH.sub.2 SO.sub.2 NMe.sub.2                                                                            Ga                                                   CH.sub.2 SO.sub.2 NMeEt  Ga                                                   CH.sub.2 SO.sub.2 NEt.sub.2                                                                            Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 NMe.sub.2                                                                   Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 NMeEt                                                                       Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 NEt.sub.2                                                                   Ga                                                   CH.sub.2 SO.sub.2 N(OMe)Me                                                                             Ga                                                   CH.sub.2 SO.sub.2 N(OMe)Et                                                                             Ga                                                   CH.sub.2 SO.sub.2 N(OEt)Me                                                                             Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 N(OMe)Me                                                                    Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 N(OMe)Et                                                                    Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 N(OEt)Me                                                                    Ga                                                   CH.sub.2 CONHMe          Ga                                                   CH.sub.2 COMHEt          Ga                                                   CH.sub.2 CONHPr-n        Gb                                                   CH.sub.2 CH.sub.2 CONHMe Ga                                                   CH.sub.2 CH.sub.2 CONHEt Ga                                                   CH.sub.2 CH.sub.2 CONHPr-n                                                                             Gb                                                   CH.sub.2 CONMe.sub.2     Ga                                                   CH.sub.2 CONMeEt         Ga                                                   CH.sub. 2 CONEt.sub.2    Ga                                                   CH.sub.2 CONHOMe         Ga                                                   CH.sub.2 CONHOEt         Ga                                                   CH.sub.2 CONHOPr-n       Gb                                                   CH.sub.2 CON(OMe)Me      Ga                                                   CH.sub.2 CON(OMe)Et      Ga                                                   CH.sub.2 CON(OEt)Me      Ga                                                   CH.sub.2 CON(OEt)Et      Ga                                                   CH.sub.2 NHMe            Ga                                                   CH.sub.2 NHEt            Ga                                                   CH.sub.2 NHPr-n          Gb                                                   CH.sub.2 CH.sub.2 NHMe   Ga                                                   CH.sub.2 CH.sub.2 NHEt   Ga                                                   CH.sub.2 CH.sub.2 NHPr-n Gb                                                   CH.sub.2 NHOMe           Ga                                                   CH.sub.2 NHOEt           Ga                                                   CH.sub.2 CH.sub.2 NHOMe  Ga                                                   CH.sub.2 CH.sub.2 NHOEt  Ga                                                   CH.sub.2 NMe.sub.2       Ga                                                   CH.sub.2 NMeEt           Ga                                                   CH.sub.2 CH.sub.2 NMe.sub.2                                                                            Ga                                                   CH.sub.2 CH.sub.2 NMeEt  Ga                                                   CH.sub.2 N(OMe)Me        Ga                                                   CH.sub.2 N(OMe)Et        Ga                                                   CH.sub.2 N(OEt)Me        Ga                                                   CH.sub.2 CH.sub.2 N(OMe)Me                                                                             Ga                                                   CH.sub.2 CH.sub.2 N(OMe)Et                                                                             Ga                                                   CH.sub.2 CH.sub.2 N(OEt)Me                                                                             Ga                                                   CH.sub.2 NMeCOMe         Ga                                                   CH.sub.2 NEtCOMe         Ga                                                   CH.sub.2 NMeCOEt         Ga                                                   CH.sub.2 CH.sub.2 NMeCOMe                                                                              Ga                                                   CH.sub.2 CH.sub.2 NEtCOMe                                                                              Ga                                                   CH.sub.2 CH.sub.2 NMeCOEt                                                                              Ga                                                   CH.sub.2 N(OMe)COMe      Ga                                                   CH.sub.2 N(OEt)COMe      Ga                                                   CH.sub.2 N(OMe)COEt      Ga                                                   CH.sub.2 CH.sub.2 N(OMe)COMe                                                                           Ga                                                   CH.sub.2 CH.sub.2 N(OEt)COMe                                                                           Ga                                                   CH.sub.2 CH.sub.2 N(OMe)COEt                                                                           Ga                                                   CH.sub.2 NMeSO.sub.2 Me  Ga                                                   CH.sub.2 NEtSO.sub.2 Me  Ga                                                   CH.sub.2 NMeSO.sub.2 Et  Ga                                                   CH.sub.2 CH.sub.2 NMeSO.sub.2 Me                                                                       Ga                                                   CH.sub.2 CH.sub.2 NEtSO.sub.2 Me                                                                       Ga                                                   CH.sub.2 CH.sub.2 NMeSO.sub.2 Et                                                                       Ga                                                   CH.sub.2 N(OMe)SO.sub.2 Me                                                                             Ga                                                   CH.sub.2 N(OEt)SO.sub.2 Me                                                                             Ga                                                   CH.sub.2 N(OMe)SO.sub.2 Et                                                                             Ga                                                   CH.sub.2 CH.sub.2 N(OMe)SO.sub.2 Me                                                                    Ga                                                   CH.sub.2 CH.sub.2 N(OEt)SO.sub.2 Me                                                                    Ga                                                   CH.sub.2 CH.sub.2 N(OMe)SO.sub.2 Et                                                                    Ga                                                   CH.sub.2 Ph              Gb                                                   CH.sub.2 CH.sub.2 Ph     Gb                                                   CH.sub.2 CH.sub.2 CH.sub.2 Ph                                                                          Gb                                                   CHMePh                   Gb                                                   CH.sub.2 CHCHPh          Ga                                                   CHMeCHCHPh               Ga                                                   CH.sub.2 CCPh            Ga                                                   CHMeCCPh                 Ga                                                   CH.sub.2 CH.sub.2 OPh    Ga                                                   CH.sub.2 OPh             Ga                                                   CH.sub.2 CH.sub.2 SPh    Ga                                                   CH.sub.2 SPh             Ga                                                   CH.sub.2 CH.sub.2 SOPh   Gb                                                   CH.sub.2 CH.sub.2 SO.sub.2 Ph                                                                          Ga                                                   CH.sub.2 OCH.sub.2 Ph    Ga                                                   CH.sub.2 CH.sub.2 OCH.sub.2 Ph                                                                         Ga                                                   CH.sub.2 SCH.sub.2 Ph    Ga                                                   CH.sub.2 CH.sub.2 SCH.sub.2 Ph                                                                         Ga                                                   CH.sub.2 SOCH.sub.2 Ph   Gb                                                   CH.sub.2 CH.sub.2 SOCH.sub.2 Ph                                                                        Gb                                                   CH.sub.2 SO.sub.2 CH.sub.2 Ph                                                                          Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 CH.sub.2 Ph                                                                 Ga                                                   CH.sub.2 COPh            Ga                                                   CH.sub.2 CH.sub.2 COPh   Ga                                                   CHMeCOPh                 Ga                                                   CH.sub.2 COCH.sub.2 Ph   Gb                                                   CHMeCOCH.sub.2 Ph        Gb                                                   CH.sub.2 CH.sub.2 CH.sub.2 F                                                                           Ga                                                   CH.sub.2 CH.sub.2 CH.sub.2 Cl                                                                          Ga                                                   CH.sub.2 C(Cl)CH.sub.2   Ga                                                   Ph                       Ga                                                   CH.sub.2 SOPh            Ga                                                   CH.sub.2 SO.sub.2 Ph     Ga                                                   CH.sub.2 C(Cl)CHCl       Ga                                                   CH.sub.2 C(F)CHCl        Ga                                                   CH.sub.2 CHCHF           Ga                                                   CH.sub.2 C(Cl)CHMe       Ga                                                   CH.sub.2 CHC(Cl)Me       Ga                                                   CH.sub.2 CFCF.sub.2      Ga                                                   CH.sub.2 CHCHCH.sub.2 F  Ga                                                   CH.sub.2 C(Br)CHMe       Ga                                                   CH.sub.2 C(Cl)CHF        Ga                                                   CH.sub.2 C(Br)CHF        Ga                                                   CH.sub.2 C(Cl)C(Cl)Me    Ga                                                   CH.sub.2 C(Br)CHBr       Ga                                                   CH.sub.2 C(Br)C(Br)Me    Ga                                                   CH.sub.2 CHC(F)CF.sub.3  Ga                                                   CH.sub.2 CHCCl.sub.2     Ga                                                   CH.sub.2 C(F)CH.sub.2    Ga                                                   CH.sub.2 CHC(F)Cl        Ga                                                   CH.sub.2 C(Cl)C(F)Cl     Ga                                                   CH.sub.2 C(F)CCl.sub.2   Ga                                                   CH.sub.2 C(Cl)CF.sub.2   Ga                                                   CH.sub.2 C(CF.sub.3)CH.sub.2                                                                           Ga                                                   CH.sub.2 CHCHI           Ga                                                   CH.sub.2 CHCBr.sub.2     Ga                                                   CH.sub.2 C(F)CHBr        Ga                                                   CH.sub.2 C(I)CH.sub.2    Ga                                                   CH.sub.2 C(Cl)CCl.sub.2  Ga                                                   CH.sub.2 C(F)C(Cl)CF.sub.3                                                                             Ga                                                   CH.sub.2 CHC(F)CF.sub.2 Cl                                                                             Ga                                                   CH.sub.2 C(Br)CH.sub.2   Ga                                                   CH.sub.2 NHSO.sub.2 Me   Gb                                                   CH.sub.2 CH.sub.2 NHSO.sub.2 Me                                                                        Gb                                                   CH.sub.2 NHCOMe          Gb                                                   CH.sub.2 CH.sub.2 NHCOMe Gb                                                   ______________________________________                                    

                  TABLE 2B                                                        ______________________________________                                         ##STR353##                                                                    ##STR354##                                                                    ##STR355##                                                                    ##STR356##                                                                    ##STR357##                                                                    ##STR358##                                                                    ##STR359##                                                                    ##STR360##                                                                    ##STR361##                                                                    ##STR362##                                                                    ##STR363##                                                                    ##STR364##                                                                    ##STR365##                                                                    ##STR366##                                                                    ##STR367##                                                                   R.sup.c1                 Gn                                                   ______________________________________                                        Me                       Ga                                                   Et                       Ga                                                   Pr-n                     Ga                                                   Pr-iso                   Ga                                                   Bu-n                     Ga                                                   Bu-iso                   Gb                                                   Pen-n                    Gb                                                   Hex-n                    Gb                                                   CH.sub.2 Pr-cyc          Ga                                                   CH.sub.2 CH.sub.2 Pr-cyc Ga                                                   CH.sub.2 CHCH.sub.2      Ga                                                   CH.sub.2 CHCHMe          Ga                                                   CH.sub.2 CCH             Ga                                                   CH.sub.2 CCMe            Ga                                                   CH.sub.2 OMe             Ga                                                   CH.sub.2 OEt             Ga                                                   CH.sub.2 CH.sub.2 OMe    Ga                                                   CH.sub.2 CH.sub.2 OEt    Ga                                                   CH.sub.2 OCH.sub.2 CHCH.sub.2                                                                          Ga                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CHCH.sub.2                                                                 Ga                                                   CH.sub.2 OCH.sub.2 CCH   Ga                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CCH                                                                        Ga                                                   CH.sub.2 OCH.sub.2 CF.sub.3                                                                            Ga                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CF.sub.3                                                                   Ga                                                   CH.sub.2 SMe             Ga                                                   CH.sub.2 SEt             Ga                                                   CH.sub.2 CH.sub.2 SMe    Ga                                                   CH.sub.2 CH.sub.2 SEt    Ga                                                   CH.sub.2 SO.sub.2 Me     Ga                                                   CH.sub.2 SO.sub.2 Et     Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 Me                                                                          Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 Et                                                                          Ga                                                   CH.sub.2 CH.sub.2 F      Ga                                                   CH.sub.2 CF.sub.3        Ga                                                   CH.sub.2 CN              Ga                                                   CH.sub.2 CH.sub.2 CN     Ga                                                   CHMeCN                   Ga                                                   CH.sub.2 CHCHCN          Ga                                                   CH.sub.2 NO.sub.2        Ga                                                   CH.sub.2 CH.sub.2 NO.sub.2                                                                             Ga                                                   CH.sub.2 CO.sub.2 Me     Gb                                                   CH.sub.2 CO.sub.2 Et     Gb                                                   CHMeCO.sub.2 Me          Gb                                                   CHMeCO.sub.2 Et          Gb                                                   CH.sub.2 CH.sub.2 CO.sub.2 Me                                                                          Ga                                                   CH.sub.2 CH.sub.2 CO.sub.2 Et                                                                          Ga                                                   CH.sub.2 CHCHCO.sub.2 Me Ga                                                   CH.sub.2 CHCHCO.sub.2 Et Ga                                                   CHMeCHCHCO.sub.2 Me      Ga                                                   CH.sub.2 COMe            Ga                                                   CH.sub.2 COEt            Ga                                                   CH.sub.2 COPr-n          Gb                                                   CH.sub.2 COCF.sub.3      Ga                                                   CH.sub.2 COCHCH.sub.2    Ga                                                   CH.sub.2 COCHCHMe        Ga                                                   CH.sub.2 COCH.sub.2 OMe  Ga                                                   CH.sub.2 COCH.sub.2 OEt  Ga                                                   CH.sub.2 COCH.sub.2 CH.sub. 2 OMe                                                                      Ga                                                   CH.sub.2 COCH.sub.2 CH.sub.2 OEt                                                                       Ga                                                   CH.sub.2 COCH.sub.2 SMe  Ga                                                   CH.sub.2 COCH.sub.2 CH.sub.2 SMe                                                                       Ga                                                   CH.sub.2 COCH.sub.2 SO.sub.2 Me                                                                        Ga                                                   CH.sub.2 COCH.sub.2 CH.sub.2 SO.sub.2 Me                                                               Ga                                                   CH.sub.2 CHCHCOMe        Ga                                                   CHMeCHCHCOMe             Ga                                                   CH.sub.2 SO.sub.2 NHMe   Gb                                                   CH.sub.2 CH.sub.2 SO.sub.2 NHMe                                                                        Gb                                                   CH.sub.2 SO.sub.2 NHMe   Gb                                                   CH.sub.2 CH.sub.2 SO.sub.2 NHOMe                                                                       Gb                                                   CH.sub.2 SO.sub.2 NMe.sub.2                                                                            Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 NMe.sub.2                                                                   Ga                                                   CH.sub.2 SO.sub.2 N(OMe)Me                                                                             Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 N(OMe)Me                                                                    Ga                                                   CH.sub.2 CONHMe          Gb                                                   CH.sub.2 CH.sub.2 CONHMe Gb                                                   CH.sub.2 CONMe.sub.2     Ga                                                   CH.sub.2 CH.sub.2 CONMe.sub.2                                                                          Ga                                                   CH.sub.2 CONHOMe         Gb                                                   CH.sub.2 CH.sub.2 CONHOMe                                                                              Gb                                                   CH.sub.2 CON(OMe)Me      Ga                                                   CH.sub.2 CH.sub.2 CON(OMe)Me                                                                           Ga                                                   CH.sub.2 NHMe            Gb                                                   CH.sub.2 CH.sub.2 NHMe   Gb                                                   CH.sub.2 NHOMe           Gb                                                   CH.sub.2 CH.sub.2 NHOMe  Gb                                                   CH.sub.2 NMe.sub.2       Ga                                                   CH.sub.2 CH.sub.2 NMe.sub.2                                                                            Ga                                                   CH.sub.2 N(OMe)Me        Ga                                                   CH.sub.2 CH.sub.2 N(OMe)Me                                                                             Ga                                                   CH.sub.2 NMeCOMe         Ga                                                   CH.sub.2 CH.sub. 2 NMeCOMe                                                                             Ga                                                   CH.sub.2 N(OMe)COMe      Ga                                                   CH.sub.2 CH.sub.2 N(OMe)COMe                                                                           Ga                                                   CH.sub.2 NMeSO.sub.2 Me  Ga                                                   CH.sub.2 CH.sub.2 NMeSO.sub.2 Me                                                                       Ga                                                   CH.sub.2 N(OMe)SO.sub.2 Me                                                                             Ga                                                   CH.sub.2 CH.sub.2 N(OMe)SO.sub.2 Me                                                                    Ga                                                   CH.sub.2 Ph              Gb                                                   CH.sub.2 CH.sub.2 Ph     Gb                                                   CH.sub.2 CH.sub.2 CH.sub.2 Ph                                                                          Gb                                                   CHMePh                   Gb                                                   CH.sub.2 CHCHPh          Gb                                                   CHMeCHCHPh               Gb                                                   CH.sub.2 CH.sub.2 OPh    Gb                                                   CH.sub.2 OPh             Gb                                                   CH.sub.2 CH.sub.2 SPh    Gb                                                   CH.sub.2 SPh             Gb                                                   CH.sub.2 CH.sub.2 SO.sub.2 Ph                                                                          Gb                                                   CH.sub.2 COPh            Gb                                                   CH.sub.2 CH.sub.2 COPh   Gb                                                   CH.sub.2 COCH.sub.2 Ph   Gb                                                   CH.sub.2 CH.sub.2 COCH.sub.2 Ph                                                                        Gb                                                   Ph                       Ga                                                   ______________________________________                                    

                  TABLE 2C                                                        ______________________________________                                         ##STR368##                                                                   Q:                                                                                 ##STR369##                                                                    ##STR370##                                                                    ##STR371##                                                                    ##STR372##                                                                    ##STR373##                                                                    ##STR374##                                                                    ##STR375##                                                                    ##STR376##                                                                    ##STR377##                                                                    ##STR378##                                                                    ##STR379##                                                                    ##STR380##                                                                    ##STR381##                                                                    ##STR382##                                                                    ##STR383##                                                                    ##STR384##                                                                    ##STR385##                                                                    ##STR386##                                                                    ##STR387##                                                                    ##STR388##                                                                    ##STR389##                                                                    ##STR390##                                                                    ##STR391##                                                                    ##STR392##                                                                    ##STR393##                                                                    ##STR394##                                                                    ##STR395##                                                                    ##STR396##                                                                    ##STR397##                                                                    ##STR398##                                                                    ##STR399##                                                                    ##STR400##                                                                    ##STR401##                                                                    ##STR402##                                                                    ##STR403##                                                                    ##STR404##                                                                    ##STR405##                                                                    ##STR406##                                                                    ##STR407##                                                                    ##STR408##                                                                    ##STR409##                                                                    ##STR410##                                                                    ##STR411##                                                                    ##STR412##                                                                    ##STR413##                                                                    ##STR414##                                                                    ##STR415##                                                                    ##STR416##                                                                    ##STR417##                                                                    ##STR418##                                                                    ##STR419##                                                                    ##STR420##                                                                    ##STR421##                                                                    ##STR422##                                                                    ##STR423##                                                                    ##STR424##                                                                    ##STR425##                                                                    ##STR426##                                                                    ##STR427##                                                                    ##STR428##                                                                    ##STR429##                                                                    ##STR430##                                                                    ##STR431##                                                                    ##STR432##                                                                    ##STR433##                                                                    ##STR434##                                                                    ##STR435##                                                                    ##STR436##                                                                    ##STR437##                                                                    ##STR438##                                                                    ##STR439##                                                                    ##STR440##                                                                    ##STR441##                                                                    ##STR442##                                                                    ##STR443##                                                                    ##STR444##                                                                    ##STR445##                                                                    ##STR446##                                                                    ##STR447##                                                                    ##STR448##                                                                    ##STR449##                                                                    ##STR450##                                                                    ##STR451##                                                                    ##STR452##                                                                    ##STR453##                                                                    ##STR454##                                                                    ##STR455##                                                                    ##STR456##                                                                    ##STR457##                                                                    ##STR458##                                                                    ##STR459##                                                                    ##STR460##                                                                    ##STR461##                                                                    ##STR462##                                                                    ##STR463##                                                                    ##STR464##                                                                    ##STR465##                                                                    ##STR466##                                                                    ##STR467##                                                                    ##STR468##                                                                    ##STR469##                                                                    ##STR470##                                                                    ##STR471##                                                                    ##STR472##                                                                    ##STR473##                                                                    ##STR474##                                                                    ##STR475##                                                                    ##STR476##                                                               ______________________________________                                        R.sup.c1          Gn                                                          ______________________________________                                        Me                Ga                                                          Et                Ga                                                          Pr-n              Ga                                                          Pro-iso           Gb                                                          Bu-n              Ga                                                          Bu-iso            Ga                                                          Pen-n             Gb                                                          CH.sub.2 Pr-cyc   Ga                                                          CH.sub.2 CH.sub.2 Pr-cyc                                                                        Gb                                                          CH.sub.2 CHCH.sub.2                                                                             Ga                                                          CH.sub.2 CHCHMe   Ga                                                          CH.sub.2 CCH      Ga                                                          CH.sub.2 CCMe     Ga                                                          CH.sub.2 CH.sub.2 OMe                                                                           Ga                                                          CH.sub.2 OMe      Ga                                                          CH.sub.2 CH.sub.2 SMe                                                                           Ga                                                          CH.sub.2 SMe      Ga                                                          CH.sub.2 SO.sub.2 Me                                                                            Ga                                                          CH.sub.2 CH.sub.2 SO.sub.2 Me                                                                   Ga                                                          CH.sub.2 CF.sub.3 Ga                                                          CH.sub.2 CN       Ga                                                          CH.sub.2 CH.sub.2 CN                                                                            Ga                                                          CH.sub.2 NO.sub.2 Ga                                                          CH.sub.2 CH.sub.2 NO.sub.2                                                                      Ga                                                          CH.sub.2 COMe     Ga                                                          CH.sub.2 COEt     Ga                                                          CH.sub.2 COCHCH.sub.2                                                                           Ga                                                          CH.sub.2 CHCHCOMe Ga                                                          CH.sub.2 CONMe.sub.2                                                                            Ga                                                          Ph                Ga                                                          ______________________________________                                    

                  TABLE 3                                                         ______________________________________                                         ##STR477##                                                                   Q:                                                                                 ##STR478##                                                                    ##STR479##                                                                    ##STR480##                                                                    ##STR481##                                                                    ##STR482##                                                                    ##STR483##                                                                    ##STR484##                                                                    ##STR485##                                                                    ##STR486##                                                                    ##STR487##                                                                    ##STR488##                                                                    ##STR489##                                                                    ##STR490##                                                                    ##STR491##                                                                    ##STR492##                                                                    ##STR493##                                                                    ##STR494##                                                                    ##STR495##                                                                    ##STR496##                                                                    ##STR497##                                                                    ##STR498##                                                                    ##STR499##                                                                    ##STR500##                                                                    ##STR501##                                                                    ##STR502##                                                                    ##STR503##                                                                    ##STR504##                                                                    ##STR505##                                                                    ##STR506##                                                                    ##STR507##                                                                    ##STR508##                                                                    ##STR509##                                                                    ##STR510##                                                                    ##STR511##                                                                    ##STR512##                                                                    ##STR513##                                                                    ##STR514##                                                                    ##STR515##                                                                    ##STR516##                                                                    ##STR517##                                                                    ##STR518##                                                                    ##STR519##                                                                    ##STR520##                                                                    ##STR521##                                                                    ##STR522##                                                                    ##STR523##                                                                    ##STR524##                                                                    ##STR525##                                                                    ##STR526##                                                                    ##STR527##                                                                    ##STR528##                                                                    ##STR529##                                                                    ##STR530##                                                                    ##STR531##                                                                    ##STR532##                                                                    ##STR533##                                                                    ##STR534##                                                                    ##STR535##                                                                    ##STR536##                                                                    ##STR537##                                                                    ##STR538##                                                                    ##STR539##                                                                    ##STR540##                                                               ______________________________________                                        R.sup.n           Gn                                                          ______________________________________                                        Me                Ga                                                          Et                Ga                                                          Pr-n              Ga                                                          Pr-iso            Gb                                                          Bu-n              Gb                                                          Pen-n             Gb                                                          Hex-n             Gb                                                          CH.sub.2 CHCH.sub.2                                                                             Ga                                                          CH.sub.2 CHCHMe   Ga                                                          CH.sub.2 CHCMe.sub.2                                                                            Gb                                                          CHMeCHCH.sub.2    Gb                                                          CH.sub.2 CCH      Ga                                                          CH.sub.2 CCMe     Ga                                                          CHMeCCH           Gb                                                          CH.sub.2 SMe      Ga                                                          CH.sub.2 SEt      Ga                                                          CH.sub.2 SPr-n    Gb                                                          CH.sub.2 CH.sub.2 SMe                                                                           Ga                                                          CH.sub.2 CH.sub.2 SEt                                                                           Ga                                                          CH.sub.2 SOMe     Gb                                                          CH.sub.2 SOEt     Gb                                                          CH.sub.2 CH.sub.2 SOMe                                                                          Gb                                                          CH.sub.2 CH.sub.2 SOEt                                                                          Gb                                                          CH.sub.2 SO.sub.2 Me                                                                            Ga                                                          CH.sub.2 SO.sub.2 Et                                                                            Ga                                                          CH.sub.2 SO.sub.2 Pr-n                                                                          Gb                                                          CH.sub.2 CH.sub.2 SO.sub.2 Me                                                                   Ga                                                          CH.sub.2 CH.sub.2 SO.sub.2 Et                                                                   Ga                                                          CH.sub.2 OMe      Ga                                                          CH.sub.2 OEt      Ga                                                          CH.sub.2 OPr-n    Gb                                                          CH.sub.2 CH.sub.2 OMe                                                                           Ga                                                          CH.sub.2 CH.sub.2 OEt                                                                           Ga                                                          CH.sub.2 CH.sub.2 OPr-n                                                                         Gb                                                          CH.sub.2 CO.sub.2 Me                                                                            Ga                                                          CH.sub.2 CO.sub.2 Et                                                                            Ga                                                          CHMeCO.sub.2 Me   Ga                                                          CHMeCO.sub.2 Et   Ga                                                          CH.sub.2 COMe     Ga                                                          CH.sub.2 COEt     Ga                                                          CH.sub.2 COPr-n   Gb                                                          CH.sub.2 CH.sub.2 COMe                                                                          Ga                                                          CH.sub.2 CH.sub.2 COEt                                                                          Ga                                                          CH.sub.2 CN       Ga                                                          CH.sub.2 CH.sub.2 CN                                                                            Ga                                                          CH.sub.2 CH.sub.2 CH.sub.2 CN                                                                   Ga                                                          Ph                Ga                                                          CH.sub.2 Ph       Ga                                                          CH.sub.2 CH.sub.2 Ph                                                                            Ga                                                          CHMePh            Ga                                                          ______________________________________                                         R.sup.n represents R.sup.d6 or R.sup.f2.                                 

                  TABLE 4A                                                        ______________________________________                                         ##STR541##                                                                    ##STR542##                                                                    ##STR543##                                                                    ##STR544##                                                                    ##STR545##                                                                    ##STR546##                                                                    ##STR547##                                                                    ##STR548##                                                                    ##STR549##                                                                    ##STR550##                                                                    ##STR551##                                                                    ##STR552##                                                                    ##STR553##                                                                    ##STR554##                                                                    ##STR555##                                                                    ##STR556##                                                                    ##STR557##                                                                    ##STR558##                                                                    ##STR559##                                                                    ##STR560##                                                                   R.sup.g1                 Gn                                                   ______________________________________                                        Me                       Ga                                                   Et                       Ga                                                   Pr-n                     Ga                                                   Pr-iso                   Ga                                                   Bu-n                     Ga                                                   Bu-iso                   Ga                                                   Bu-sec                   Gb                                                   Bu-tert                  Gb                                                   Pen-n                    Ga                                                   Hex-n                    Gb                                                   Hep-n                    Gb                                                   Pr-cyc                   Ga                                                   Hex-cyc                  Ga                                                   CH.sub.2 Pr-cyc          Ga                                                   CH.sub.2 CH.sub.2 Pr-cyc Ga                                                   CH.sub.2 Bu-cyc          Gb                                                   CH.sub.2 Pen-cyc         Gc                                                   Hexen-cyc                Gb                                                   CH.sub.2 Penten-cyc      Gb                                                   CH.sub.2 CHCH.sub.2      Ga                                                   CH.sub.2 CHCHMe          Ga                                                   CH.sub.2 CHCHEt          Ga                                                   CH.sub.2 CHCMe.sub.2     Gb                                                   CH.sub.2 CMeCH.sub.2     Gb                                                   CH.sub.2 CMeCHCHMe       Gc                                                   CH.sub.2 CH.sub.2 CHCH.sub.2                                                                           Gb                                                   CH.sub.2 CH.sub.2 CHCHMe Gb                                                   CH.sub.2 CCH             Ga                                                   CH.sub.2 CCMe            Ga                                                   CH.sub.2 CCEt            Ga                                                   CH.sub.2 CH.sub.2 CCH    Gb                                                   CH.sub.2 CH.sub.2 CCMe   Gb                                                   CHMeCCH                  Gb                                                   CHMeC CMe                Gc                                                   CH.sub.2 OMe             Ga                                                   CH.sub.2 OEt             Ga                                                   CH.sub.2 OPr-n           Gb                                                   CH.sub.2 CH.sub.2 OMe    Ga                                                   CH.sub.2 CH.sub.2 OEt    Ga                                                   CH.sub.2 CH.sub.2 OPr-n  Gb                                                   CH.sub.2 CHMeOMe         Gb                                                   CH.sub.2 CH.sub.2 CH.sub.2 OMe                                                                         Ga                                                   CH.sub.2 CH.sub.2 CH.sub.2 OEt                                                                         Ga                                                   CH.sub.2 OCH.sub.2 CHCH.sub.2                                                                          Ga                                                   CH.sub.2 OCH.sub.2 CHCHMe                                                                              Ga                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CHCH.sub.2                                                                 Ga                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CHCHMe                                                                     Ga                                                   CH.sub.2 OCH.sub.2 CCH   Ga                                                   CH.sub.2 OCH.sub.2 CCMe  Ga                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CCH                                                                        Ga                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CCMe                                                                       Ga                                                   CH.sub.2 OCHF.sub.2      Ga                                                   CH.sub.2 OCF.sub.3       Ga                                                   CH.sub.2 CH.sub.2 OCHF.sub.2                                                                           Ga                                                   CH.sub.2 CH.sub.2 OCF.sub.3                                                                            Ga                                                   CH.sub.2 OCH.sub.2 CF.sub.3                                                                            Ga                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CF.sub.3                                                                   Ga                                                   CH.sub.2 OCH.sub.2 CH.sub.2 F                                                                          Ga                                                   CH.sub.2 OCH.sub.2 CH.sub.2 Cl                                                                         Ga                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 F                                                                 Ga                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 Cl                                                                Ga                                                   CH.sub.2 OCH.sub.2 CHCHCl                                                                              Gb                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CHCHCl                                                                     Gb                                                   CH.sub.2 OCH.sub.2 CHCHBr                                                                              Gb                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CHCHBr                                                                     Gb                                                   CH.sub.2 OCH.sub.2 CHCF.sub.2                                                                          Gb                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CHCF.sub.2                                                                 Gb                                                   CH.sub.2 OCH.sub.2 CHCHCF.sub.3                                                                        Gb                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CHCHCF.sub.3                                                               Gb                                                   CH.sub.2 OCH.sub.2 CCI   Gb                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CCI                                                                        Gb                                                   CH.sub.2 OCH.sub.2 CCCF.sub.3                                                                          Gb                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CCCF.sub.3                                                                 Gb                                                   CH.sub.2 SMe             Ga                                                   CH.sub.2 SEt             Ga                                                   CH.sub.2 SPr-n           Gb                                                   CH.sub.2 CH.sub.2 SMe    Ga                                                   CH.sub.2 CH.sub.2 SEt    Ga                                                   CH.sub.2 CH.sub.2 SPr-n  Gb                                                   CH.sub.2 SOMe            Gb                                                   CH.sub.2 SOEt            Gb                                                   CH.sub.2 CH.sub.2 SOMe   Gb                                                   CH.sub.2 CH.sub.2 SOEt   Gb                                                   CH.sub.2 SO.sub.2 Me     Ga                                                   CH.sub.2 SO.sub.2 Et     Ga                                                   CH.sub.2 SO.sub.2 Pr-n   Gb                                                   CH.sub.2 CH.sub.2 SO.sub.2 Me                                                                          Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 Et                                                                          Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 Pr-n                                                                        Gb                                                   CH.sub.2 CH.sub.2 F      Ga                                                   CH.sub.2 CHF.sub.2       Ga                                                   CH.sub.2 CF.sub.3        Ga                                                   CH.sub.2 CH.sub.2 Cl     Ga                                                   CH.sub.2 CH.sub.2 Br     Ga                                                   CH.sub.2 CH.sub.2 CF.sub.3                                                                             Ga                                                   CH.sub.2 CF.sub.2 CF.sub.3                                                                             Ga                                                   CH.sub.2 CHCHCl          Gb                                                   CH.sub.2 CHCHBr          Gb                                                   CH.sub.2 CHCF.sub.2      Gb                                                   CH.sub.2 CHCHCF.sub.3    Gb                                                   CH.sub.2 CCI             Gb                                                   CH.sub.2 CCCF.sub.3      Gb                                                   CH.sub.2 CN              Ga                                                   CH.sub.2 CH.sub.2 CN     Ga                                                   CHMeCN                   Ga                                                   CH.sub.2 CHCHCN          Ga                                                   CH(CN)CCH                Gb                                                   CH.sub.2 NO.sub.2        Ga                                                   CH.sub.2 CH.sub.2 NO.sub.2                                                                             Ga                                                   CH.sub.2 CHCHNO.sub.2    Gb                                                   CH.sub.2 CH(NO.sub.2)CHCH.sub.2                                                                        Gc                                                   CH.sub.2 CH(NO.sub.2)CCH Gc                                                   CH.sub.2 CO.sub.2 Me     Gb                                                   CH.sub.2 CO.sub.2 Et     Gb                                                   CH.sub.2 CO.sub.2 Pr-n   Gb                                                   CHMeCO.sub.2 Me          Gb                                                   CHMeCO.sub.2 Et          Gb                                                   CH.sub.2 CH.sub.2 CO.sub.2 Me                                                                          Ga                                                   CH.sub.2 CH.sub.2 CO.sub.2 Et                                                                          Ga                                                   CH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 Me                                                                 Gb                                                   CH.sub.2 CHCHCO.sub.2 Me Ga                                                   CH.sub.2 CHCHCO.sub.2 Et Ga                                                   CHMeCHCHCO.sub.2 Me      Ga                                                   CHMeCHCHCO.sub.2 Et      Ga                                                   CH.sub.2 CCCO.sub.2 Me   Ga                                                   CH.sub.2 CCCO.sub.2 Et   Ga                                                   CH.sub.2 COMe            Ga                                                   CH.sub.2 COEt            Ga                                                   CH.sub.2 COPr-n          Gb                                                   CH.sub.2 CH.sub.2 COMe   Ga                                                   CH.sub.2 CH.sub.2 COEt   Ga                                                   CH.sub.2 COCF.sub.3      Ga                                                   CH.sub.2 CH.sub.2 COCF.sub.3                                                                           Ga                                                   CH.sub.2 COCH.sub.2 CF.sub.3                                                                           Gb                                                   CH.sub.2 COCH.sub.2 F    Gb                                                   CH.sub.2 COCHCH.sub.2    Ga                                                   CH.sub.2 COCHCHMe        Ga                                                   CH.sub.2 COCH.sub.2 CHCH.sub.2                                                                         Gb                                                   CH.sub.2 CH.sub.2 COCHCH.sub.2                                                                         Gb                                                   CH.sub.2 CH.sub.2 COCHCHMe                                                                             Gb                                                   CH.sub.2 COCCH           Ga                                                   CH.sub.2 COCCMe          Ga                                                   CH.sub.2 COCH.sub.2 OMe  Ga                                                   CH.sub.2 COCH.sub.2 OEt  Ga                                                   CH.sub.2 COCH.sub.2 CH.sub.2 OMe                                                                       Ga                                                   CH.sub.2 COCH.sub.2 CH.sub.2 OEt                                                                       Ga                                                   CH.sub.2 COCH.sub.2 SMe  Ga                                                   CH.sub.2 COCH.sub.2 SEt  Ga                                                   CH.sub.2 COCH.sub.2 CH.sub.2 SMe                                                                       Ga                                                   CH.sub.2 COCH.sub.2 CH.sub.2 SEt                                                                       Ga                                                   CH.sub.2 COCH.sub.2 SOMe Gb                                                   CH.sub.2 COCH.sub.2 CH.sub.2 SOMe                                                                      Gb                                                   CH.sub.2 COCH.sub.2 SO.sub.2 Me                                                                        Ga                                                   CH.sub.2 COCH.sub.2 SO.sub.2 Et                                                                        Ga                                                   CH.sub.2 COCH.sub.2 CH.sub.2 SO.sub.2 Me                                                               Ga                                                   CH.sub.2 COCH.sub.2 CH.sub.2 SO.sub.2 Et                                                               Ga                                                   CH.sub.2 CHCHCOMe        Ga                                                   CH.sub.2 CHCHCOEt        Ga                                                   CHMeCHCHCOMe             Ga                                                   CHMeCHCHCOEt             Ga                                                   CH.sub.2 CCCOMe          Ga                                                   CH.sub.2 C CCOEt         Ga                                                   CH.sub.2 SO.sub.2 NHMe   Ga                                                   CH.sub.2 SO.sub.2 NHEt   Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 NHMe                                                                        Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 NHEt                                                                        Ga                                                   CH.sub.2 SO.sub.2 NHOMe  Ga                                                   CH.sub.2 SO.sub.2 NHOEt  Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 NHOMe                                                                       Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 NHOEt                                                                       Ga                                                   CH.sub.2 SO.sub.2 NMe.sub.2                                                                            Ga                                                   CH.sub.2 SO.sub.2 NMeEt  Ga                                                   CH.sub.2 SO.sub.2 NEt.sub.2                                                                            Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 NMe.sub.2                                                                   Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 NMeEt                                                                       Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 NEt.sub.2                                                                   Ga                                                   CH.sub.2 SO.sub.2 N(OMe)Me                                                                             Ga                                                   CH.sub.2 SO.sub.2 N(OMe)Et                                                                             Ga                                                   CH.sub.2 SO.sub.2 N(OEt)Me                                                                             Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 N(OMe)Me                                                                    Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 N(OMe)Et                                                                    Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 N(OEt)Me                                                                    Ga                                                   CH.sub.2 CONHMe          Ga                                                   CH.sub.2 CONHEt          Ga                                                   CH.sub.2 CONHPr-n        Gb                                                   CH.sub.2 CH.sub.2 CONHMe Ga                                                   CH.sub.2 CH.sub.2 CONHEt Ga                                                   CH.sub.2 CH.sub.2 CONHPr-n                                                                             Gb                                                   CH.sub.2 CONMe.sub.2     Ga                                                   CH.sub.2 CONMeEt         Ga                                                   CH.sub.2 CONEt.sub.2     Ga                                                   CH.sub. 2 CONHOMe        Ga                                                   CH.sub.2 CONHOEt         Ga                                                   CH.sub.2 CONHOPr-n       Gb                                                   CH.sub.2 CON(OMe)Me      Ga                                                   CH.sub.2 CON(OMe)Et      Ga                                                   CH.sub.2 CON(OEt)Me      Ga                                                   CH.sub.2 CON(OEt)Et      Ga                                                   CH.sub.2 NHMe            Ga                                                   CH.sub.2 NHEt            Ga                                                   CH.sub.2 NHPr-n          Gb                                                   CH.sub.2 CH.sub.2 NHMe   Ga                                                   CH.sub.2 CH.sub.2 NHEt   Ga                                                   CH.sub.2 CH.sub.2 NHPr-n Gb                                                   CH.sub.2 NHOMe           Ga                                                   CH.sub.2 NHOEt           Ga                                                   CH.sub.2 CH.sub.2 NHOMe  Ga                                                   CH.sub.2 CH.sub.2 NHOEt  Ga                                                   CH.sub.2 NMe.sub.2       Ga                                                   CH.sub.2 NMeEt           Ga                                                   CH.sub.2 CH.sub.2 NMe.sub.2                                                                            Ga                                                   CH.sub.2 CH.sub.2 NMeEt  Ga                                                   CH.sub.2 N(OMe)Me        Ga                                                   CH.sub.2 N(OMe)Et        Ga                                                   CH.sub.2 N(OEt)Me        Ga                                                   CH.sub.2 CH.sub.2 N(OMe)Me                                                                             Ga                                                   CH.sub.2 CH.sub.2 N(OMe)Et                                                                             Ga                                                   CH.sub.2 CH.sub.2 N(OEt)Me                                                                             Ga                                                   CH.sub.2 NMeCOMe         Ga                                                   CH.sub.2 NEtCOMe         Ga                                                   CH.sub.2 NMeCOEt         Ga                                                   CH.sub.2 CH.sub.2 NMeCOMe                                                                              Ga                                                   CH.sub.2 CH.sub.2 NEtCOMe                                                                              Ga                                                   CH.sub.2 CH.sub.2 NMeCOEt                                                                              Ga                                                   CH.sub.2 N(OMe)COMe      Ga                                                   CH.sub.2 N(OEt)COMe      Ga                                                   CH.sub.2 N(OMe)COEt      Ga                                                   CH.sub.2 CH.sub.2 N(OMe)COMe                                                                           Ga                                                   CH.sub.2 CH.sub.2 N(OEt)COMe                                                                           Ga                                                   CH.sub.2 CH.sub.2 N(OMe)COEt                                                                           Ga                                                   CH.sub.2 NMeSO.sub.2 Me  Ga                                                   CH.sub.2 NEtSO.sub.2 Me  Ga                                                   CH.sub.2 NMeSO.sub.2 Et  Ga                                                   CH.sub.2 CH.sub.2 NMeSO.sub.2 Me                                                                       Ga                                                   CH.sub.2 CH.sub.2 NEtSO.sub.2 Me                                                                       Ga                                                   CH.sub.2 CH.sub.2 NMeSO.sub.2 Et                                                                       Ga                                                   CH.sub.2 N(OMe)SO.sub.2 Me                                                                             Ga                                                   CH.sub.2 N(OEt)SO.sub.2 Me                                                                             Ga                                                   CH.sub.2 N(OMe)SO.sub.2 Et                                                                             Ga                                                   CH.sub.2 CH.sub.2 N(OMe)SO.sub.2 Me                                                                    Ga                                                   CH.sub.2 CH.sub.2 N(OEt)SO.sub.2 Me                                                                    Ga                                                   CH.sub.2 CH.sub.2 N(OMe)SO.sub.2 Et                                                                    Ga                                                   CH.sub.2 Ph              Gb                                                   CH.sub.2 CH.sub.2 Ph     Gb                                                   CH.sub.2 CH.sub.2 CH.sub.2 Ph                                                                          Gb                                                   CHMePh                   Gb                                                   CH.sub.2 CHCHPh          Ga                                                   CHMeCHCHPh               Ga                                                   CH.sub.2 CCPh            Ga                                                   CHMeCCPh                 Ga                                                   CH.sub.2 CH.sub.2 OPh    Ga                                                   CH.sub.2 OPh             Ga                                                   CH.sub.2 CH.sub.2 SPh    Ga                                                   CH.sub.2 SPh             Ga                                                   CH.sub.2 CH.sub.2 SOPh   Gb                                                   CH.sub.2 CH.sub.2 SO.sub.2 Ph                                                                          Ga                                                   CH.sub.2 OCH.sub.2 Ph    Ga                                                   CH.sub.2 CH.sub.2 OCH.sub.2 Ph                                                                         Ga                                                   CH.sub.2 SCH.sub.2 Ph    Ga                                                   CH.sub.2 CH.sub.2 SCH.sub.2 Ph                                                                         Ga                                                   CH.sub.2 SOCH.sub.2 Ph   Gb                                                   CH.sub.2 CH.sub. 2 SOCH.sub.2 Ph                                                                       Gb                                                   CH.sub.2 SO.sub.2 CH.sub.2 Ph                                                                          Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 CH.sub.2 Ph                                                                 Ga                                                   CH.sub.2 COPh            Ga                                                   CH.sub.2 CH.sub.2 COPh   Ga                                                   CHMeCOPh                 Ga                                                   CH.sub.2 COCH.sub.2 Ph   Gb                                                   CHMeCOCH.sub.2 Ph        Gb                                                   CH.sub.2 CH.sub.2 CH.sub.2 F                                                                           Ga                                                   CH.sub.2 CH.sub.2 CH.sub.2 Cl                                                                          Ga                                                   ______________________________________                                    

                  TABLE 4B                                                        ______________________________________                                         ##STR561##                                                                    ##STR562##                                                                    ##STR563##                                                                    ##STR564##                                                                    ##STR565##                                                                    ##STR566##                                                                    ##STR567##                                                                    ##STR568##                                                                    ##STR569##                                                                    ##STR570##                                                                    ##STR571##                                                                    ##STR572##                                                                    ##STR573##                                                                    ##STR574##                                                                    ##STR575##                                                                    ##STR576##                                                                    ##STR577##                                                                    ##STR578##                                                                   R.sup.g1                 Gn                                                   ______________________________________                                        Me                       Ga                                                   Et                       Ga                                                   Pr-n                     Ga                                                   Pr-iso                   Ga                                                   Bu-n                     Ga                                                   Bu-iso                   Gb                                                   Pen-n                    Gb                                                   Hex-n                    Gb                                                   CH.sub.2 Pr-cyc          Ga                                                   CH.sub.2 CH.sub.2 Pr-cyc Ga                                                   CH.sub.2 CHCH.sub.2      Ga                                                   CH.sub.2 CHCHMe          Ga                                                   CH.sub.2 CCH             Ga                                                   CH.sub.2 CCMe            Ga                                                   CH.sub.2 OMe             Ga                                                   CH.sub.2 OEt             Ga                                                   CH.sub.2 CH.sub.2 OMe    Ga                                                   CH.sub.2 CH.sub.2 OEt    Ga                                                   CH.sub.2 OCH.sub.2 CHCH.sub.2                                                                          Ga                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CHCH.sub.2                                                                 Ga                                                   CH.sub.2 OCH.sub.2 CCH   Ga                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CCH                                                                        Ga                                                   CH.sub.2 OCH.sub.2 CF.sub.3                                                                            Ga                                                   CH.sub.2 CH.sub.2 OCH.sub.2 CF.sub.3                                                                   Ga                                                   CH.sub.2 SMe             Ga                                                   CH.sub.2 SEt             Ga                                                   CH.sub.2 CH.sub.2 SMe    Ga                                                   CH.sub.2 CH.sub.2 SEt    Ga                                                   CH.sub.2 SO.sub.2 Me     Ga                                                   CH.sub.2 SO.sub.2 Et     Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 Me                                                                          Ga                                                   CH.sub.2 CH.sub.2 CO.sub.2 Et                                                                          Ga                                                   CH.sub.2 CH.sub.2 F      Ga                                                   CH.sub.2 CF.sub.3        Ga                                                   CH.sub.2 CN              Ga                                                   CH.sub.2 CH.sub.2 CN     Ga                                                   CHMeCN                   Ga                                                   CH.sub.2 CHCHCN          Ga                                                   CH.sub.2 NO.sub.2        Ga                                                   CH.sub.2 CH.sub.2 NO.sub.2                                                                             Ga                                                   CH.sub.2 CO.sub.2 Me     Gb                                                   CH.sub.2 CO.sub.2 Et     Gb                                                   CHMeCO.sub.2 Me          Gb                                                   CHMeCO.sub.2 Et          Gb                                                   CH.sub.2 CH.sub.2 CO.sub.2 Me                                                                          Ga                                                   CH.sub.2 CH.sub.2 CO.sub.2 Et                                                                          Ga                                                   CH.sub.2 CHCHCO.sub.2 Me Ga                                                   CH.sub.2 CHCHCO.sub.2 Et Ga                                                   CHMeCHCHCO.sub.2 Me      Ga                                                   CH.sub.2 COMe            Ga                                                   CH.sub.2 COEt            Ga                                                   CH.sub.2 COPr-n          Gb                                                   CH.sub.2 COCF.sub.3      Ga                                                   CH.sub.2 COCHCH.sub.2    Ga                                                   CH.sub.2 COCHCHMe        Ga                                                   CH.sub.2 COCH.sub.2 OMe  Ga                                                   CH.sub.2 COCH.sub.2 OEt  Ga                                                   CH.sub.2 COCH.sub.2 CH.sub.2 OMe                                                                       Ga                                                   CH.sub.2 COCH.sub.2 CH.sub.2 OEt                                                                       Ga                                                   CH.sub.2 COCH.sub.2 SMe  Ga                                                   CH.sub.2 COCH.sub.2 CH.sub.2 SMe                                                                       Ga                                                   CH.sub.2 COCH.sub.2 SO.sub.2 Me                                                                        Ga                                                   CH.sub.2 COCH.sub.2 CH.sub.2 SO.sub.2 Me                                                               Ga                                                   CH.sub.2 CHCHCOMe        Ga                                                   CHMeCHCHCOMe             Ga                                                   CH.sub.2 SO.sub.2 NHMe   Gb                                                   CH.sub.2 CH.sub.2 SO.sub.2 NHMe                                                                        Gb                                                   CH.sub.2 SO.sub.2 NHOMe  Gb                                                   CH.sub.2 CH.sub.2 SO.sub.2 NHOMe                                                                       Gb                                                   CH.sub.2 SO.sub.2 NMe.sub.2                                                                            Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 NMe.sub.2                                                                   Ga                                                   CH.sub.2 SO.sub.2 N(OMe)Me                                                                             Ga                                                   CH.sub.2 CH.sub.2 SO.sub.2 N(OMe)Me                                                                    Ga                                                   CH.sub.2 CONHMe          Gb                                                   CH.sub.2 CH.sub.2 CONHMe Gb                                                   CH.sub.2 CONMe.sub.2     Ga                                                   CH.sub.2 CH.sub.2 CONMe.sub.2                                                                          Ga                                                   CH.sub.2 CONHOMe         Gb                                                   CH.sub.2 CH.sub.2 CONHOMe                                                                              Gb                                                   CH.sub.2 CON(OMe)Me      Ga                                                   CH.sub.2 CH.sub.2 CON(OMe)Me                                                                           Ga                                                   CH.sub.2 NHMe            Gb                                                   CH.sub.2 CH.sub.2 NHMe   Gb                                                   CH.sub.2 NHOMe           Gb                                                   CH.sub.2 CH.sub.2 NHOMe  Gb                                                   CH.sub.2 NMe.sub.2       Ga                                                   CH.sub.2 CH.sub.2 NMe.sub.2                                                                            Ga                                                   CH.sub.2 N(OMe)Me        Ga                                                   CH.sub.2 CH.sub.2 N(OMe)Me                                                                             Ga                                                   CH.sub.2 NMeCOMe         Ga                                                   CH.sub.2 CH.sub.2 NMeCOMe                                                                              Ga                                                   CH.sub.2 N(OMe)COMe      Ga                                                   CH.sub.2 CH.sub.2 N(OMe)COMe                                                                           Ga                                                   CH.sub.2 NMeSO.sub.2 Me  Ga                                                   CH.sub.2 CH.sub.2 NMeSO.sub.2 Me                                                                       Ga                                                   CH.sub.2 N(OMe)SO.sub.2 Me                                                                             Ga                                                   CH.sub.2 CH.sub.2 N(OMe)SO.sub.2 Me                                                                    Ga                                                   CH.sub.2 Ph              Gb                                                   CH.sub.2 CH.sub.2 Ph     Gb                                                   CH.sub.2 CH.sub.2 CH.sub.2 Ph                                                                          Gb                                                   CHMePh                   Gb                                                   CH.sub.2 CHCHPh          Gb                                                   CHMeCHCHPh               Gb                                                   CH.sub.2 CH.sub.2 OPh    Gb                                                   CH.sub.2 OPh             Gb                                                   CH.sub.2 CH.sub.2 SPh    Gb                                                   CH.sub.2 SPh             Gb                                                   CH.sub.2 CH.sub.2 SO.sub.2 Ph                                                                          Gb                                                   CH.sub.2 COPh            Gb                                                   CH.sub.2 CH.sub.2 COPh   Gb                                                   CH.sub.2 COCH.sub.2 Ph   Gb                                                   CH.sub.2 CH.sub.2 COCH.sub.2 Ph                                                                        Gb                                                   ______________________________________                                    

                  TABLE 4C                                                        ______________________________________                                         ##STR579##                                                                    ##STR580##                                                                    ##STR581##                                                                    ##STR582##                                                                    ##STR583##                                                                   R.sup.g1                Gn                                                    ______________________________________                                        Me                      Ga                                                    Et                      Ga                                                    Pr-n                    Ga                                                    Pro-iso                 Gb                                                    Bu-n                    Ga                                                    Bu-iso                  Ga                                                    Pen-n                   Gb                                                    CH.sub.2 Pr-cyc         Ga                                                    CH.sub.2 CH.sub.2 Pr-cyc                                                                              Gb                                                    CH.sub.2 CHCH.sub.2     Ga                                                    CH.sub.2 CHCHMe         Ga                                                    CH.sub.2 CCH            Ga                                                    CH.sub.2 CCMe           Ga                                                    CH.sub.2 CH.sub.2 OMe   Ga                                                    CH.sub.2 OMe            Ga                                                    CH.sub.2 CH.sub.2 SMe   Ga                                                    CH.sub.2 SMe            Ga                                                    CH.sub.2 SO.sub.2 Me    Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 Me                                                                         Ga                                                    CH.sub.2 CF.sub.3       Ga                                                    CH.sub.2 CN             Ga                                                    CH.sub.2 CH.sub.2 CN    Ga                                                    CH.sub.2 NO.sub.2       Ga                                                    CH.sub.2 CH.sub.2 NO.sub.2                                                                            Ga                                                    CH.sub.2 COMe           Ga                                                    CH.sub.2 COEt           Ga                                                    CH.sub.2 COCHCH.sub.2   Ga                                                    CH.sub.2 CHCHCOMe       Ga                                                    CH.sub.2 CONMe.sub.2    Ga                                                    ______________________________________                                    

                  TABLE 5                                                         ______________________________________                                         ##STR584##                                                                   Q:                                                                                 ##STR585##                                                                    ##STR586##                                                                    ##STR587##                                                                    ##STR588##                                                                    ##STR589##                                                                    ##STR590##                                                                    ##STR591##                                                                    ##STR592##                                                                    ##STR593##                                                                    ##STR594##                                                                    ##STR595##                                                                    ##STR596##                                                                    ##STR597##                                                                    ##STR598##                                                                    ##STR599##                                                                    ##STR600##                                                                    ##STR601##                                                                    ##STR602##                                                                    ##STR603##                                                                    ##STR604##                                                                    ##STR605##                                                                    ##STR606##                                                                    ##STR607##                                                                    ##STR608##                                                                    ##STR609##                                                                    ##STR610##                                                                    ##STR611##                                                                    ##STR612##                                                                    ##STR613##                                                                    ##STR614##                                                                    ##STR615##                                                                    ##STR616##                                                                    ##STR617##                                                                    ##STR618##                                                                    ##STR619##                                                                    ##STR620##                                                                    ##STR621##                                                                    ##STR622##                                                                    ##STR623##                                                                    ##STR624##                                                                    ##STR625##                                                                    ##STR626##                                                                    ##STR627##                                                                    ##STR628##                                                                    ##STR629##                                                                    ##STR630##                                                                    ##STR631##                                                                    ##STR632##                                                                    ##STR633##                                                                    ##STR634##                                                                    ##STR635##                                                                    ##STR636##                                                                    ##STR637##                                                               ______________________________________                                        R.sup.m          L           Gn                                               ______________________________________                                        Me               Me          Ga                                               Me               Et          Gb                                               Et               Me          Ga                                               Et               Et          Gb                                               Pr-n             Me          Ga                                               Pr-n             Et          Gb                                               Pr-n             CH.sub.2 CHCH.sub.2                                                                       Gb                                               Pr-n             CH.sub.2 CCH                                                                              Gb                                               Bu-n             Me          Ga                                               Bu-n             Et          Gb                                               Bu-n             CH.sub.2 CHCH.sub.2                                                                       Gb                                               Bu-n             CH.sub.2 CCH                                                                              Gb                                               Pen-n            Me          Gb                                               CH.sub.2 CHCH.sub.2                                                                            Me          Ga                                               CH.sub.2 CHCH.sub.2                                                                            Et          Gb                                               CH.sub.2 CHCH.sub.2                                                                            CH.sub.2 CHCH.sub.2                                                                       Gb                                               CH.sub.2 CHCH.sub.2                                                                            CH.sub.2 CCH                                                                              Gb                                               CH.sub.2 CCH     Me          Gb                                               CH.sub.2 CCH     Et          Gb                                               CH.sub.2 CCH     CH.sub.2 CHCH.sub.2                                                                       Gb                                               CH.sub.2 CCH     CH.sub.2 CCH                                                                              Gb                                               CH.sub.2 CH.sub.2 OMe                                                                          Me          Gb                                               CH.sub.2 CH.sub.2 SMe                                                                          Me          Gb                                               CH.sub.2 S0.sub.2 Me                                                                           Me          Gb                                               CH.sub.2 CF.sub.3                                                                              Me          Gb                                               CH.sub.2 CF.sub.3                                                                              Et          Gb                                               CH.sub.2 CF.sub.3                                                                              CH.sub.2 CHCH.sub.2                                                                       Gb                                               CH.sub.2 CF.sub.3                                                                              CH.sub.2 CCH                                                                              Gb                                               CH.sub.2 CN      Me          Gb                                               CH.sub.2 COMe    Me          Gb                                               CH.sub.2 COMe    Et          Gb                                               CH.sub.2 COMe    CH.sub.2 CHCH.sub.2                                                                       Gb                                               CH.sub.2 COMe    CH.sub.2 CCH                                                                              Gb                                               CH.sub.2 COCHCH.sub.2                                                                          Me          Gb                                               CH.sub.2 CONMe.sub.2                                                                           Me          Gb                                               ______________________________________                                         R.sup.m represents R.sup.a1, R.sup.b1, R.sup.d1, R.sup.e1 , or R.sup.f1. 

                  TABLE 6                                                         ______________________________________                                         ##STR638##                                                                   Q:                                                                                 ##STR639##                                                                    ##STR640##                                                                    ##STR641##                                                                    ##STR642##                                                                    ##STR643##                                                                    ##STR644##                                                                    ##STR645##                                                                    ##STR646##                                                                    ##STR647##                                                                    ##STR648##                                                                    ##STR649##                                                                    ##STR650##                                                                    ##STR651##                                                                    ##STR652##                                                                    ##STR653##                                                                    ##STR654##                                                                    ##STR655##                                                                    ##STR656##                                                               ______________________________________                                        R.sup.c1        L              Gn                                             ______________________________________                                        Me              Me             Ga                                             Me              Et             Gb                                             Me              CH.sub.2 CHCH.sub.2                                                                          Gb                                             Me              CH.sub.2 CCH   Gb                                             Et              Me             Ga                                             Et              Et             Gb                                             Et              CH.sub.2 CHCH.sub.2                                                                          Gb                                             Et              CH.sub.2 CCH   Gb                                             Pr-n            Me             Ga                                             Pr-n            Et             Gb                                             Bu-n            Me             Ga                                             Bu-n            Et             Gb                                             Pen-n           Me             Gb                                             CH.sub.2 CHCH.sub.2                                                                           Me             Ga                                             CH.sub.2 CHCH.sub.2                                                                           Et             Gb                                             CH.sub.2 CHCH.sub.2                                                                           CH.sub.2 CHCH.sub.2                                                                          Gb                                             CH.sub.2 CHCH.sub.2                                                                           CH.sub.2 CCH   Gb                                             CH.sub.2 CCH    Me             Gb                                             CH.sub.2 CCH    Et             Gb                                             CH.sub.2 CCH    CH.sub.2 CHCH.sub.2                                                                          Gb                                             CH.sub.2 CCH    CH.sub.2 CCH   Gb                                             CH.sub.2 CH.sub.2 OMe                                                                         Me             Gb                                             CH.sub.2 CH.sub.2 SMe                                                                         Me             Gb                                             CH.sub.2 SO.sub.2 Me                                                                          Me             Gb                                             CH.sub.2 CF.sub.3                                                                             Me             Gb                                             CH.sub.2 CF.sub.3                                                                             Et             Gb                                             CH.sub.2 CF.sub.3                                                                             CH.sub.2 CHCH.sub.2                                                                          Gb                                             CH.sub.2 CF.sub.3                                                                             CH.sub.2 CCH   Gb                                             CH.sub.2 CN     Me             Gb                                             CH.sub.2 COMe   Me             Gb                                             CH.sub.2 COMe   Et             Gb                                             CH.sub.2 COMe   CH.sub.2 CHCH.sub.2                                                                          Gb                                             CH.sub.2 COMe   CH.sub.2 CCH   Gb                                             CH.sub.2 COCHCH.sub.2                                                                         Me             Gb                                             CH.sub.2 CONMe.sub.2                                                                          Me             Gb                                             Ph              Me             Gb                                             ______________________________________                                    

                  TABLE 7                                                         ______________________________________                                         ##STR657##                                                                   Q:                                                                                 ##STR658##                                                                    ##STR659##                                                                    ##STR660##                                                                    ##STR661##                                                                    ##STR662##                                                                    ##STR663##                                                                    ##STR664##                                                                    ##STR665##                                                                    ##STR666##                                                                    ##STR667##                                                                    ##STR668##                                                                    ##STR669##                                                                    ##STR670##                                                                    ##STR671##                                                                    ##STR672##                                                                    ##STR673##                                                                    ##STR674##                                                                    ##STR675##                                                                    ##STR676##                                                                    ##STR677##                                                                    ##STR678##                                                                    ##STR679##                                                                    ##STR680##                                                                    ##STR681##                                                                    ##STR682##                                                                    ##STR683##                                                               ______________________________________                                        R.sup.n         L              Gn                                             ______________________________________                                        Me              Me             Ga                                             Me              Et             Gb                                             Me              CH.sub.2 CHCH.sub.2                                                                          Gb                                             Me              CH.sub.2 CCH   Gb                                             Et              Me             Ga                                             Et              Et             Gb                                             Et              CH.sub.2 CHCH.sub.2                                                                          Gb                                             Et              CH.sub.2 CCH   Gb                                             Pr-n            Me             Ga                                             Pr-n            Et             Gb                                             Pr-n            CH.sub.2 CHCH.sub.2                                                                          Gb                                             Pr-n            CH.sub.2 CCH   Gb                                             CH.sub.2 CHCH.sub.2                                                                           Me             Gb                                             CH.sub.2 CCH    Me             Gb                                             CH.sub.2 SMe    Me             Gb                                             CH.sub.2 CH.sub.2 SMe                                                                         Me             Gb                                             CH.sub.2 SO.sub.2 Me                                                                          Me             Gb                                             CH.sub.2 CH.sub.2 SO.sub.2 Me                                                                 Me             Gb                                             CH.sub.2 OMe    Me             Gb                                             CH.sub.2 CH.sub.2 OMe                                                                         Me             Gb                                             CH.sub.2 CO.sub.2 Me                                                                          Me             Gb                                             CH.sub.2 COMe   Me             Gb                                             CH.sub.2 CH.sub.2 COMe                                                                        Me             Gb                                             CH.sub.2 CN     Me             Gb                                             CH.sub.2 CH.sub.2 CN                                                                          Me             Gb                                             Ph              Me             Gb                                             CH.sub.2 Ph     Me             Gb                                             CH.sub.2 CH.sub.2 Ph                                                                          Me             Gb                                             CHMePh          Me             Gb                                             ______________________________________                                          R.sup.n represents R.sup.d6 or R.sup.f2.                                

                  TABLE 8                                                         ______________________________________                                         ##STR684##                                                                   Q:                                                                                 ##STR685##                                                                    ##STR686##                                                                    ##STR687##                                                                    ##STR688##                                                                    ##STR689##                                                                    ##STR690##                                                                    ##STR691##                                                                    ##STR692##                                                                    ##STR693##                                                                    ##STR694##                                                                    ##STR695##                                                                    ##STR696##                                                                    ##STR697##                                                               ______________________________________                                        R.sup.g1        L              Gn                                             ______________________________________                                        Me              Me             Ga                                             Me              Et             Gb                                             Et              Me             Ga                                             Et              Et             Gb                                             Pr-n            Me             Ga                                             Pr-n            Et             Gb                                             Pr-n            CH.sub.2 CHCH.sub.2                                                                          Gb                                             Pr-n            CH.sub.2 CCH   Gb                                             Bu-n            Me             Ga                                             Bu-n            Et             Gb                                             Bu-n            CH.sub.2 CHCH.sub.2                                                                          Gb                                             Bu-n            CH.sub.2 CCH   Gb                                             Pen-n           Me             Gb                                             CH.sub.2 CHCH.sub.2                                                                           Me             Ga                                             CH.sub.2 CHCH.sub.2                                                                           Et             Gb                                             CH.sub.2 CHCH.sub.2                                                                           CH.sub. 2 CHCH.sub.2                                                                         Gb                                             CH.sub.2 CHCH.sub.2                                                                           CH.sub.2 CCH   Gb                                             CH.sub.2 CCH    Me             Gb                                             CH.sub.2 CCH    Et             Gb                                             CH.sub.2 CCH    CH.sub.2 CHCH.sub.2                                                                          Gb                                             CH.sub.2 CCH    CH.sub.2 CCH   Gb                                             CH.sub.2 CH.sub.2 OMe                                                                         Me             Gb                                             CH.sub.2 CH.sub.2 SMe                                                                         Me             Gb                                             CH.sub.2 SO.sub.2 Me                                                                          Me             Gb                                             CH.sub.2 CF.sub.3                                                                             Me             Gb                                             CH.sub.2 CF.sub.3                                                                             Et             Gb                                             CH.sub.2 CF.sub.3                                                                             CH.sub.2 CHCH.sub.2                                                                          Gb                                             CH.sub.2 CF.sub.3                                                                             CH.sub.2 CCH   Gb                                             CH.sub.2 CN     Me             Gb                                             CH.sub.2 COMe   Me             GB                                             CH.sub.2 COMe   Et             Gb                                             CH.sub.2 COMe   CH.sub.2 CHCH.sub.2                                                                          Gb                                             CH.sub.2 COMe   CH.sub.2 C CH  Gb                                             CH.sub.2 COCHCH.sub.2                                                                         Me             Gb                                             CH.sub.2 CONMe.sub.2                                                                          Me             Gb                                             ______________________________________                                    

                  TABLE 9                                                         ______________________________________                                         ##STR698##                                                                   Q:                                                                                 ##STR699##                                                                    ##STR700##                                                                    ##STR701##                                                                    ##STR702##                                                                    ##STR703##                                                                    ##STR704##                                                                    ##STR705##                                                                    ##STR706##                                                                    ##STR707##                                                               ______________________________________                                        R.sup.m                 Gn                                                    ______________________________________                                        Me                      Gc                                                    Et                      Gc                                                    Pr-n                    Gc                                                    Pr-iso                  Gc                                                    Bu-n                    Gc                                                    Bu-iso                  Gc                                                    Pen-n                   Gc                                                    CH.sub.2 Pr-cyc         Gc                                                    CH.sub.2 CH.sub.2 Py-cyc                                                                              Gc                                                    CH.sub.2 CHCH.sub.2     Gc                                                    CH.sub.2 CHCHMe         Gc                                                    CH.sub.2 CCH            Gc                                                    CH.sub.2 CCMe           Gc                                                    CH.sub.2 CH.sub.2 OMe   Gc                                                    CH.sub.2 OMe            Gc                                                    CH.sub.2 CH.sub.2 SMe   Gc                                                    CH.sub.2 SMe            Gc                                                    CH.sub.2 SO.sub.2 Me    Gc                                                    CH.sub.2 CH.sub.2 SO.sub.2 Me                                                                         Gc                                                    CH.sub.2 CF.sub.3       Gc                                                    CH.sub.2 CN             Gc                                                    CH.sub.2 CH.sub.2 CN    Gc                                                    CH.sub.2 NO.sub.2       Gc                                                    CH.sub.2 CH.sub.2 NO.sub.2                                                                            Gc                                                    CH.sub.2 COMe           Gc                                                    CH.sub.2 COEt           Gc                                                    CH.sub.2 COCHCH.sub.2   Gc                                                    CH.sub.2 CHCHCOMe       Gc                                                    CH.sub.2 CONMe.sub.2    Gc                                                    ______________________________________                                         R.sup.m represents R.sup.a1, R.sup.b1, R.sup.d1, R.sup.e1 or R.sup.f1.   

                  TABLE 10                                                        ______________________________________                                         ##STR708##                                                                    ##STR709##                                                                    ##STR710##                                                                   R.sup.c1                Gn                                                    ______________________________________                                        Me                      Gc                                                    Et                      Gc                                                    Pr-n                    Gc                                                    Pr-iso                  Gc                                                    Bu-n                    Gc                                                    Bu-iso                  Gc                                                    Pen-n                   Gc                                                    CH.sub.2 Pr-cyc         Gc                                                    CH.sub.2 CH.sub.2 Py-cyc                                                                              Gc                                                    CH.sub.2 CHCH.sub.2     Gc                                                    CH.sub.2 CHCHMe         Gc                                                    CH.sub.2 CCH            Gc                                                    CH.sub.2 C CMe          Gc                                                    CH.sub.2 CH.sub.2 OMe   Gc                                                    CH.sub.2 OMe            Gc                                                    CH.sub.2 CH.sub.2 SMe   Gc                                                    CH.sub.2 SMe            Gc                                                    CH.sub.2 SO.sub.2 Me    Gc                                                    CH.sub.2 CH.sub.2 SO.sub.2 Me                                                                         Gc                                                    CH.sub.2 CF.sub.3       Gc                                                    CH.sub.2 CN             Gc                                                    CH.sub.2 CH.sub.2 CN    Gc                                                    CH.sub.2 NO.sub.2       Gc                                                    CH.sub.2 CH.sub.2 NO.sub.2                                                                            Gc                                                    CH.sub.2 COMe           Gc                                                    CH.sub.2 COEt           Gc                                                    CH.sub.2 COCHCH.sub.2   Gc                                                    CH.sub.2 CHCHCOMe       Gc                                                    CH.sub.2 CONMe.sub.2    Gc                                                    Ph                      Gc                                                    ______________________________________                                    

                  TABLE 11                                                        ______________________________________                                         ##STR711##                                                                    ##STR712##                                                                    ##STR713##                                                                    ##STR714##                                                                   R.sup.n represents R.sup.d6 or R.sup.f2.                                      Rn                      Gn                                                    ______________________________________                                        Me                      Gc                                                    Et                      Gc                                                    Pr-n                    Gc                                                    CH.sub.2 CHCH.sub.2     Gc                                                    CH.sub.2 CCH            Gc                                                    CH.sub.2 SMe            Gc                                                    CH.sub.2 CH.sub.2 SMe   Gc                                                    CH.sub.2 SO.sub.2 Me    Gc                                                    CH.sub.2 CH.sub.2 SO.sub.2 Me                                                                         Gc                                                    CH.sub.2 OMe            Gc                                                    CH.sub.2 CH.sub.2 OMe   Gc                                                    CH.sub.2 CO.sub.2 Me    Gc                                                    CH.sub.2 COMe           Gc                                                    CH.sub.2 CH.sub.2 COMe  Gc                                                    CH.sub.2 CN             Cc                                                    CH.sub.2 CH.sub.2 CN    Gc                                                    Ph                      Gc                                                    CH.sub.2 Ph             Gc                                                    ______________________________________                                    

                  TABLE 12                                                        ______________________________________                                         ##STR715##                                                                    ##STR716##                                                                    ##STR717##                                                                    ##STR718##                                                                    ##STR719##                                                                    ##STR720##                                                                   R.sup.g1                Gn                                                    ______________________________________                                        Me                      Gc                                                    Et                      Gc                                                    Pr-n                    Gc                                                    Pr-iso                  Gc                                                    Bu-n                    Gc                                                    Bu-iso                  Gc                                                    Pen-n                   Gc                                                    CH.sub.2 Pr-cyc         Gc                                                    CH.sub.2 CH.sub.2 Py-cyc                                                                              Gc                                                    CH.sub.2 CHCH.sub.2     Gc                                                    CH.sub.2 CHCHMe         Gc                                                    CH.sub.2 CCH            Gc                                                    CH.sub.2 CCMe           Gc                                                    CH.sub.2 CH.sub.2 OMe   Gc                                                    CH.sub.2 OMe            Gc                                                    CH.sub.2 CH.sub.2 SMe   Gc                                                    CH.sub.2 SMe            Gc                                                    CH.sub.2 SO.sub.2 Me    Gc                                                    CH.sub.2 CH.sub.2 SO.sub.2 Me                                                                         Gc                                                    CH.sub.2 CF.sub.3       Gc                                                    CH.sub.2 CN             Gc                                                    CH.sub.2 CH.sub.2 CN    Gc                                                    CH.sub.2 NO.sub.2       Gc                                                    CH.sub.2 CH.sub.2 NO.sub.2                                                                            Gc                                                    CH.sub.2 COMe           Gc                                                    CH.sub.2 COEt           Gc                                                    CH.sub.2 COCHCH.sub.2   Gc                                                    CH.sub.2 CHCHCOMe       Gc                                                    CH.sub.2 CONMe.sub.2    Gc                                                    ______________________________________                                    

The compound of the present invention can be used as a herbicide forupland fields by any treating method such as soil treatment, soiladmixing treatment or foliage treatment.

The dose of the compound of the present invention varies depending uponthe application site, the season for application, the manner ofapplication, the type of weeds to be controlled, the type of cropplants, etc. However, the dose is usually within a range of from 0.0001to 10 kg, preferably from 0.005 to 5 kg, per hectare (ha), as the amountof the active ingredient.

Further, the compound of the present invention may be combined withother herbicides, various insecticides, fungicides, plant growthregulating agents, synergism agents and safeners at the time of thepreparation of the formulations or at the time of the application, asthe case requires.

Particularly, by the combined application with other herbicide, it canbe expected to reduce the cost due to a decrease of the dose or toenlarge the herbicidal spectrum or obtain higher herbicidal effects dueto a synergistic effect of the combined herbicides. In such a case, aplurality of known herbicides may be simultaneously combined. Theherbicides of the type which can be used in combination with thecompound of the present invention, may, for example, be compoundsdisclosed in Farm Chemicals Handbook (1990).

When the compound of the present invention is to be used as a herbicide,it is usually mixed with a suitable carrier, for instance, a solidcarrier such as clay, talc, bentonite, diatomaceous earth or fine silicapowder, or a liquid carrier such as water, an alcohol (such asisopropanol, butanol, benzyl alcohol or furfuryl alcohol), an aromatichydrocarbon (such as toluene or xylene), an ether (such as anisole), aketone (such as cyclohexanone or isophorone), an ester (such as butylacetate), an acid amide (such as N-methylpyrrolidone), or a halogenatedhydrocarbon (such as chlorobenzene). If desired, a surfactant, anemulsifier, a dispersing agent, a penetrating agent, a spreader, athickener, an antifreezing agent, a coagulation preventing agent or astabilizer may be added to prepare an optional formulation such as aliquid formulation, an emulsifiable concentrate, a wettable powder, adry flowable, a flowable, a dust or a granule.

Cropland weeds to be controlled by the compound of the present inventioninclude, for example, Solanaceae weeds such as Solanum nigrum and Daturastramonium, Malvaceae weeds such as Abutilon theophrasti and Sidespinosa, Convolvulaceae weeds such as Ipomoea spps. e.g. Ipomoeapurpurea, and Calystegia spps., Amaranthaceae weeds such as Amaranthuslividus and Amaranthus viridis, Compositae weeds such as Xanthiumstrumarium, Ambrosia artemisiaefolia, Helianthus annuu, Galinsogaciliat, Cirsium arvense, Senecio vulgaris and Erigeron annus, Cruciferaeweeds such as Rorippa indica, Sinapis arvensis and CapsellaBursapastris, Polygonaceae weeds such as Polygonum Blumei and Polygonumconvolvulus, Portulacaceae weeds such as Portulaca oleracea,Chenopodiaceae weeds such as Chenopodium album, Chenopodium ficifoliumand Kochia scoparis, Caryophyllaceae weeds such as Stellaria media,Scrophulariaceae weeds such as Veronica persica, Commelinaceae weedssuch as Commelina communis, Labiatae weeds such as Lamium amplexicauleand Lamium purpureum, Euphorbiaceae weeds such as Euphorbia supina andEuphorbia maculata, Rubiaceae weeds such as Galium spurium, Galiumaparine and Rubia akane, Violaceae weeds such as Viola arvensis,Leguminosae weeds such as Sesbania exaltata and Cassia obtusifolia,Graminaceous weeds such as Sorgham bicolor, Panicum dichotomiflorum,Sorghum halepense, Echinochloa crus-galli, Digitaria adscendens, Avenafatua, Eleusine indica, Setaria viridis and Alopecurus aegualis, andCyperaceous weeds such as Cyperus rotundus and Cyperus esculentus.

Further, the compound of the present invention can be used as a paddyfield herbicide by any treating method such as irrigated soil treatmentor foliage treatment. Paddy weeds include, for example, Alismataceaeweeds such as Alisma canaliculatum, Sagittaria trifolia and Sagittariapygmaea, Cyperaceae weeds such as Cyperus difformis, Cyperus serotinus,Scirpus juncoides and Eleocharis kuroguwai, Scrothulariaceae weeds suchas Lindemia pyxidaria, Potenderiaceae weeds such as Monochoriavaginalis, Potamogetonaceae weeds such as Potamogeton distinctus,Lythraceae weeds such as Rotala indica, and Gramineae weeds such asEchinochloa crus-galli.

The compound of the present invention can be applied to control variousweeds not only in the agricultural and horticultural fields such asupland fields, paddy fields or orchards, but also in non-agriculturalfields such as play grounds, non-used vacant fields or railway sides.

The compound of the present invention can easily be produced byselecting any one of the following reaction schemes 1 to 5.

Reaction Scheme 1 ##STR721## In the above formulas, Q, G and L are asdefined above, and Z is a halogen atom.

Namely, the amine (2) is reacted with chlorosulfonyl isocyanate in asolvent such as tetrahydrofuran, dimethoxyethane, acetonitrile,propionitrile, dimethylformamide, dichloromethane, dichloroethane,benzene or toluene and then reacted with the imine (3) or (4) in thepresence of a base such as triethylamine, pyridine, sodium hydride,sodium methoxide, sodium ethoxide, sodium hydroxide, potassium hydroxideor potassium carbonate, to obtain the compound of the present invention(1:X=O).

Reaction Scheme 2 ##STR722## In the above formulas, Q, G, L and Z are asdefined above, and Y is a C₁₋₆ alkyl group or a phenyl group.

Namely, the reaction of the imine (3) or (4) with phenylN-chlorosulfonyl carbamate (5:Y=phenyl group) or an alkylN-chlorosulfonyl carbamate (5:Y=lower alkyl group), is conducted byusing the carbamate derivative (5) in an amount of from 0.5 to 3.0 mols,per mol of the imine (3) or (4). Preferably, the amount is within arange of from 0.9 to 1.2 mols.

The reaction temperature may be selected optionally within a range offrom -50° C. to 100° C., but it is preferably within a range of from-20° C. to 30° C.

This reaction can be carried out by using various bases. The amount ofthe base is from 0.5 to 4.0 mols per mol of the imine (3) or (4).

A suitable base may, for example, be an organic base such astriethylamine or pyridine, a metal hydride such as sodium hydride, aninorganic base such as sodium hydroxide, potassium hydroxide orpotassium carbonate, or a metal alkoxide such as sodium methoxide orsodium ethoxide.

A suitable solvent for this reaction is a solvent inert to thisreaction, for example, an aromatic hydrocarbon such as benzene, tolueneor xylene, a halogenated hydrocarbon such as dichloromethane, chloroformor carbon tetrachloride, an ether such as ethyl ether, isopropyl ether,dioxane or tetrahydrofuran, a nitrile such as acetonitrile orpropionitrile, a hydrocarbon such as petroleum ether, petroleum benzineor n-hexane, a ketone such as acetone or methyl ethyl ketone, an estersuch as ethyl acetate, or an amide such as dimethylformamide,dimethylacetamide or hexamethyl phosphorous triamide.

These solvents may be used alone or in combination as a mixture.

Particularly preferred is an ether or an amide.

Then, the phenyl N-substituted iminosulfonyl carbamate (6:X=O, Y=phenylgroup) or the alkyl N-substituted iminosulfonyl carbamate (6:X=O,Y=lower alkyl group) and the compound (2) are heated in a solvent suchas benzene, toluene or dioxane to obtain the compound of the presentinvention (1:X=O).

Reaction Scheme 3 ##STR723## In the above formulas, Q, G, L and Y are asdefined above.

Namely, the substituted iminosulfonamide derivative (7) is reacted withthe carbamate derivative (8) in a solvent such as acetone, acetonitrileor dioxane in the presence of an inorganic base such as potassiumcarbonate or an organic base such as triethylamine or1,8-diazabicyclo[5.4.0]-7-undecene (DBU) to obtain the compound of thepresent invention (1:X=O).

Reaction Scheme 4 ##STR724## In the above formulas, Q, G, L, X and Y areas defined above.

Namely, the substituted iminosulfonamide derivative (7) is reacted withchloroformic acid (thio)ester or carbonic acid (thio)ester in a solventsuch as acetone, methyl ethyl ketone, acetonitrile, dioxane ortetrahydrofuran in the presence of a base such as potassium carbonate,triethylamine or pyridine to obtain the compound (6), which is thenheated together with the compound (2) in a solvent such as toluene,benzene or dioxane to obtain the compound of the present invention (1).

Reaction Scheme 5 ##STR725## In the above formulas, Q and G are asdefined above.

Namely, the substituted iminosulfonamide derivative (7) is reacted withthe isothiocyanate derivative (9) in a solvent such as acetone,acetonitrile, dioxane or tetrahydrofuran in the presence of an inorganicbase such as potassium carbonate or an organic base such astriethylamine or DBU, to obtain the compound of the present invention(1:X=S, L=H).

The intermediates to be used in the present invention, i.e. thesubstituted iminosulfonamide derivative (7), the phenyl N-substitutediminosulfonyl(thio)carbamate (6:Y=phenyl group) and the alkylN-substituted iminosulfonyl(thio)carbamate (6: Y=C₁₋₆ alkyl group) arealso novel compounds.

The substituted iminosulfonamide derivative (7) can be synthesized froman imine (3) or (4) by the methods of the following Reaction Schemes 6and 7.

Reaction Scheme 6 ##STR726## In the above formulas, Q and Z are asdefined above.

In the Reaction Scheme 6, the reaction of tert-butanol withchlorosulfonyl isocyanate can be conducted by a method per se known, forexample, in accordance with Japanese Unexamined Patent Publication No.101323/1975.

The reaction of the imine (3) or (4) with tert-butylsulfamoyl chlorideis carried out by using tert-butylsulfamoyl chloride in an amount offrom 0.5 to 3.0 mols per mol of the imine (3) or (4). Preferably theamount is within a range of from 0.9 to 1.2 mols.

The reaction temperature may be selected optionally within a range offrom -50° C. to 100° C. However, the temperature is preferably within arange of from -20° C. to 30° C.

This reaction can be conducted by using various bases. The amount of thebase is from 0.5 to 4.0 mols per mol of the imine (3) or (4).Preferably, the amount is within a range of from 0.8 to 2.5 mols. Asuitable base may, for example, be a metal hydride such as sodiumhydride, an organic base such as triethylamine or pyridine, an inorganicbase such as sodium hydroxide, potassium hydroxide or potassiumcarbonate, or a metal alkoxide such as sodium methoxide or sodiumethoxide.

A suitable solvent for the reaction is a solvent inert to this reaction,for example, an aromatic hydrocarbon such as benzene, toluene or xylene,a halogenated hydrocarbon such as dichloromethane, chloroform or carbontetrachloride, an ether such as ethyl ether, isopropyl ether, dioxane ortetrahydrofuran, a nitrile such as acetonitrile or propionitrile, ahydrocarbon such as petroleum ether, petroleum benzine or n-hexane, aketone such as acetone or methyl ethyl ketone, an ester such as ethylacetate, or an amide such as dimethylformamide, dimethylacetamide orhexamethylphosphorous triamide.

These solvents may be used alone or in combination as a mixture.Particularly preferred is an ether or an amide.

Reaction Scheme 7 ##STR727## In the above formulas, Q is as definedabove.

In the Reaction Scheme 7, removal of the tert-butyl group is carried outby using trifluoroacetic acid.

The amount of trifluoroacetic acid may be selected optionally within arange of an equimolar amount to an excess amount. Trifluoroacetic acidmay be used as a solvent without any particular problem.

The reaction temperature may be selected optionally within a range offrom -50° C. to 80° C. The temperature is preferably within a range offrom -20° C. to 30° C.

When a solvent is used for this reaction, a solvent inert to thisreaction, for example, an aromatic hydrocarbon such as benzene, tolueneor xylene, a halogenated hydrocarbon such as dichloromethane, chloroformor carbon tetrachloride, an ether such as ethyl ether, isopropyl ether,dioxane or tetrahydrofuran, a nitrile such as acetonitrile orpropionitrile, a hydrocarbon such as petroleum ether, petroleum benzineor n-hexane, a ketone such as acetone or methyl ethyl ketone, an estersuch as ethyl acetate, or an amide such as dimethylformamide,dimethylacetamide or hexamethylphosphorous triamide, may be used. Thesesolvents may be used alone or in combination as a mixture.

In Reaction Scheme 2, the phenyl N-chlorosulfonyl carbamate (5:Y=phenylgroup) and the alkyl N-chlorosulfonyl carbamate (5:Y=lower alkyl group)can be synthesized by a method known per se, for example, in accordancewith Chemische Berichte, vol. 96, p. 56 (1963).

The imines (3) and (4) to be used as the starting materials for theabove reaction, can be synthesized, for example, in accordance with U.S.Pat. No. 4,237,302, Journal of Chemical Society, p. 307 (1956), Chemicaland Pharmaceutical Bulletin, vol. 26, p. 3658 (1978), Journal of OrganicChemistry, vol. 30, p. 4298 (1965), East German Patent 291,757, Journalof American Chemical Society, vol. 93, p. 5552 (1971), U.S. Pat. No.4,054,652, British Patent 752,003, Chemische Berichte, vol. 92, p. 1928(1959), Journal of Medicinal Chemistry, vol. 6, p. 266 (1963), ChemicalAbstracts, vol. 64, 14171e (1966), and Belgian Patent 654,416.

As representative examples, synthetic schemes for2-imino-3-ethoxythiazolidine hydrobromide,2-imino-3-n-propoxythiazolidine hydrobromide and2-imino-3-methoxy-4,5-dimethylthiazoline hydrochloride will be shown asReaction Schemes 8, 9 and 10.

Reaction Scheme 8 ##STR728## Reaction Scheme 9 ##STR729## ReactionScheme 10

THE BEST MODE FOR CARRYING OUT THE INVENTION

Now, syntheses of the compounds of the present invention will bedescribed in detail as Reference Examples and working Examples. However,the present invention is by no means restricted to such specificExamples.

REFERENCE EXAMPLE a-1

Preparation of 2-imino-3-methylthiazol-4-ine hydroiodide ##STR731##

In 125 ml of dimethylformamide, 50 g (0.5 mol) of 2-aminothiazole wasdissolved, and 90 g (0.63 mol) of methyl iodide was added thereto atroom temperature. The mixture was further stirred at room temperaturefor 48 hours. Then, 1000 ml of ethyl acetate was added to the reactionmixture. Formed crystals were collected by filtration, washed with ethylacetate and then dried to obtain 105 g of 2-imino-3-methylthiazol-4-inehydroiodide.

Melting point: 181°-183° C.

The 2-imino-3-methylthiazol-4-ine hydroiodide was neutralized withpotassium carbonate to obtain 2-imino-3-methylthiazol-4-ine.

Boiling point 55°-60° C./1 mmHg

REFERENCE EXAMPLE a-2

Preparation of 2-imino-3-n-butylthiazolidine ##STR732##

In 25 ml of dimethylformamide, 8.2 g (80 mmol) of 2-amino-2-thiazolidinewas dissolved, and 18.4 g (100 mmol) of n-butyl iodide was added theretoat room temperature. The reaction mixture was heated and stirred at 60°C. for 10 hours and then left to cool to room temperature. The reactionmixture was added to 300 ml of ethyl acetate, and the mixture wasstirred at room temperature for 10 minutes. A formed oily substance wasseparated by decantation from the ethyl acetate solution, and the sameoperation was repeated twice. Then, ethyl acetate contained in the oilysubstance was distilled off under reduced pressure to obtain2-imino-3-n-butylthiazolidine hydroiodide as a crude product.

Then, the 2-imino-3-n-butylthiazolidine hydroiodide was stirred togetherwith 5.28 g (80 mmol) of 85% potassium hydroxide in 300 ml of methanolat room temperature for one hour. Methanol was distilled off underreduced pressure. Then, 200 ml of chloroform was added to the residue,and precipitated insoluble matters were removed by filtration.Chloroform was distilled off under reduced pressure, and 6.9 g of2-imino-3-n-butylthiazolidine was obtained by distillation under reducedpressure.

Boiling point: 85°-89° C./0.26 torr

REFERENCE EXAMPLE a-3

Preparation of 2-imino-1,3-dimethylimidazol-4-ine hydrochloride##STR733##

16.9 g (150 mmol) of creatinine was dissolved in 100 ml ofN,N-dimethylformamide. Then, 27.6 g (194 mmol) of methyl iodide wasadded thereto, and the mixture was heated to 50° C. and stirred at thattemperature for 2 hours and further at room temperature overnight. Tothe reaction mixture, 500 ml of ethyl acetate was added, and crystalswere collected by filtration. The obtained crystals were washed withethyl acetate and dried to obtain 26.2 g of2-imino-1,3-dimethylimidazolidin-4-one hydroiodide as white crystals.

Then, to 150 ml of a methanol solution containing 5.17 g (78.4 mmol) of85% potassium hydroxide, 20 g (78.4 mmol) of2-imino-1,3-dimethylimidazolidin-4-one hydroiodide was added, and themixture was stirred at room temperature for 20 minutes. The solvent wasdistilled off under reduced pressure. Then, to the residue, 200 ml ofchloroform was added, and insoluble matters were filtered off. Thefiltrate was dried over anhydrous magnesium sulfate, and the solvent wasdistilled off under reduced pressure to obtain 9.0 g of2-imino-1,3-dimethylimidazolidin-4-one.

800 mg (21.0 mmol) of lithium aluminum hydride was suspended in 20 ml ofdry tetrahydrofuran, and 200 ml of a dry tetrahydrofuran solutioncontaining 1.5 g (11.8 mmol) of 2-imino-1,3-dimethylimidazolidin-4-one,was added thereto at room temperature. The mixture was stirred at thesame temperature overnight. Then, to the reaction mixture, 10 ml ofethyl acetate and then 5 ml of water were carefully added, and insolublematters were filtered off. The filtrate was adjusted to pH 3 withconcentrated hydrochloric acid, and then the solvent was distilled offunder reduced pressure. Obtained crystals were washed with a solventmixture of ethyl ether and ethanol to obtain 1.2 g of2-imino-1,3-dimethylimidazol-4-ine hydrochloride.

Melting point: 168°-171° C.

The structures and the physical property values or characteristics ofthe compounds prepared by the same methods as the above ReferenceExamples a-1 to a-3 are presented in Tables 13a-1, 13a-2 and 13a-3.

                  TABLE 13a-1                                                     ______________________________________                                         ##STR734##                                                                                                   Physical                                                                      property values                               R.sup.a1    R.sup.a2                                                                             R.sup.a3                                                                              HZ   or characteristics                            ______________________________________                                        C.sub.2 H.sub.5                                                                           H      H       HI   m.p.  113-114° C.                      C.sub.3 H.sub.7 -n                                                                        H      H       HI   m.p.  99-101° C.                       CH.sub.2 Ph H      H       HBr  m.p.  153-155° C.                      CH.sub.2 CO.sub.2 CH.sub.3                                                                H      H       HBr  m.p.  174-177° C.                      CH.sub.2 CHCH.sub.2                                                                       H      H       HI   m.p.  113-116° C.                      CH.sub.2 CCH                                                                              H      H       HBr  m.p.  148-153° C.                      CH.sub.2 CO.sub.2 C.sub.2 H.sub.5                                                         H      H       HBr  m.p.  166-167° C.                      CH(CH.sub.3)CO.sub.2 C.sub.2 H.sub.5                                                      H      H       HBr  m.p.  138-141° C.                      CH.sub.2 COCH.sub.3                                                                       H      H       HBr  m.p.  139-141° C.                      CH.sub.3    CH.sub. 3                                                                            H       HI   m.p.  157-160° C.                      CH.sub.3    CH.sub.3                                                                             CH.sub.3                                                                              HI   m.p.  208-210° C.                      C.sub.3 H.sub.7 -n                                                                        CH.sub.3                                                                             H       HI   m.p.  166-168° C.                      C.sub.4 H.sub.9 -n                                                                        H      H       HI   m.p.  55-58° C.                        C.sub.5 H.sub.11 -n                                                                       H      H       --   b.p.  97-100° C./                                                            0.9 torr                                CH.sub.2 CHCHCH.sub.3                                                                     H      H       HBr  m.p.  127-128° C.                      CH.sub.2 CHCHPh                                                                           H      H       HBr  m.p.  125-129° C.                      CH.sub.2 CH.sub.2 OCH.sub.3                                                               H      H       HBr  m.p.  141-142° C.                      C.sub.3 H.sub.7 -n                                                                        CH.sub.3                                                                             CH.sub.3                                                                              HI   m.p.  135-138° C.                      CH.sub.3    Ph     H       HI   m.p.  235-238° C.                      CH.sub.3    H      Cl      HI   m.p.  225-228° C.                      CH.sub.2 COPh                                                                             H      H       HBr  m.p.  207-208° C.                      CH.sub.2 OCH.sub.2 Ph                                                                     H      H       HCl  m.p.  99-104° C.                       CH.sub.3    H      Br      HI   m.p.  223-225° C.                      C.sub.3 H.sub.7 -n                                                                        H      Cl      HI   m.p.  182-184° C.                      CH(CH.sub.3).sub.2                                                                        H      H       --   b.p.  75-78°  C./                                                            0.3 torr                                CH.sub.2 CN H      H       HBr  m.p.  154-155° C.                      CH.sub.2 CH(CH.sub.3).sub.2                                                               H      H       --   b.p.  78-81° C./                                                             0.3 torr                                C.sub.6 H.sub.13 -n                                                                       H      H       --   b.p.  110-112° C./                                                           0.45 torr                               CH(CH.sub.3)C.sub.2 H.sub.5                                                               H      H       --   b.p.  83-90° C./                                                             0.4 torr                                CH.sub.2 OCH.sub.3                                                                        H      H       --   b.p.  80-81° C./                                                             0.5 torr                                CH.sub.2 C(Cl)CH.sub.2                                                                    H      H       HCl  m.p.  155-159° C.                      CH.sub.2 CHCHCl                                                                           H      H       HCl  m.p.  60-66° C.                        CH.sub.2 SCH.sub.3                                                                        H      H       --   b.p.  82-85° C./                                                             0.6 torr                                CH.sub.2 C(CH.sub.3)CH.sub.2                                                              H      H       HCl  m.p.  114-118° C.                      CH.sub.2 CHC(CH.sub.3).sub.2                                                              H      H       --   b.p.  90-102° C./                                                            0.3 torr                                CH.sub.3    H      CH.sub.3                                                                              HI   m.p.  179-181° C.                      C.sub. 3 H.sub.7 -n                                                                       H      CH.sub.3                                                                              HI   m.p.  152-154° C.                      CH.sub.3    H      OCH.sub.3                                                                             HI   m.p.  158-160° C.                      CH.sub.2 PhOMe-p                                                                          H      H       HCl  m.p.  163-165° C.                      CH.sub.2 PhCl-p                                                                           H      H       HCl  m.p.  157-159° C.                      CH.sub.2 C(Br)CH.sub.2                                                                    H      H       HBr  m.p.  165-168° C.                      CH.sub.2 CH.sub.2 Ph                                                                      H      H       HBr  m.p.  144-145° C.                      CH.sub.2 OC.sub.2 H.sub.5                                                                 H      H       HCl  m.p.  95-97° C.                        CH.sub.2 CCCH.sub.3                                                                       H      H       HBr  m.p.  167-169° C.                      ______________________________________                                    

                  TABLE 13a-2                                                     ______________________________________                                         ##STR735##                                                                                                    Physical                                                                      property values                              R.sup.a1    R.sup.a4                                                                              R.sup.a5                                                                             HZ    or characteristics                           ______________________________________                                        CH.sub.3    H       H      HI    m.p. 147-150° C.                      C.sub.3 H.sub.7 -n                                                                        H       H      HI    m.p. 119-123° C.                      CH.sub.2 CHCH.sub.2                                                                       H       H      HI    m.p. 111-116° C.                      CH.sub.2 CCH                                                                              H       H      HBr   m.p. 118-122° C.                      C.sub.2 H.sub.5                                                                           H       H      --    b.p. 78-83° C./                                                             0.9 torr                                CH.sub.2 COCH.sub.3                                                                       H       H      HBr   m.p. 233-237° C.                      C.sub.5 H.sub.11 -n                                                                       H       H      --    b.p. 95-96° C./                                                             0.25 torr                               CH.sub.2 CHCHCH.sub.3                                                                     H       H      --    b.p. 85-90° C./                                                             0.2 torr                                C.sub.6 H.sub.13 -n                                                                       H       H      --    b.p. 109-110° C./                                                           0.4 torr                                CH.sub.3    H       CH.sub.3                                                                             --    Pale yellow oil                              C.sub.3 H.sub.7 -n                                                                        H       CH.sub.3                                                                             --    Pale yellow oil                              CH.sub.2 OCH.sub.3                                                                        H       H      HCl   White solid                                  CH.sub.2 C(Cl)CH.sub.2                                                                    H       H      HCl   m.p. 150-155° C.                      CH.sub.2 CHCHCl                                                                           H       H      HCl   m.p. 131-133° C.                      Ph          H       H      HCl   m.p. 224-226° C.                      ______________________________________                                    

                  TABLE 13a-3                                                     ______________________________________                                         ##STR736##                                                                                                    Physical property values                     R.sup.a1                                                                             R.sup.a2                                                                             R.sup.a3                                                                              R.sup.a6                                                                           HZ    or characteristics                           ______________________________________                                        C.sub.2 H.sub.5                                                                      H      H       CH.sub.3                                                                           HCl   Pale yellow solid                            C.sub.3 H.sub.7 -n                                                                   H      H       CH.sub.3                                                                           HCl   Pale yellow solid                            ______________________________________                                    

REFERENCE EXAMPLE b-1

Preparation of 2-imino-3-n-propylthiadiazol-4-ine hydroiodide ##STR737##

In 40 ml of dimethylformamide, 8.1 g (80 mmol) of 2-aminothiadiazole wasdissolved, and 17.0 g (100 mmol) of n-propyl iodide was added thereto atroom temperature. The mixture was heated at 60° C. for 30 minutes andthen left to cool, and then it was stirred at room temperature for 24hours. Then, to the reaction mixture, 500 ml of ethyl acetate was added.Formed crystals were collected by filtration, washed with ethyl acetateand then dried to obtain 13.1 g of desired2-imino-3-n-propylthiadiazol-4-ine hydroiodide.

Melting point: 121°-124° C.

The structures and the physical property values of the compoundsprepared by the same method as in the above Reference Example b-1 arepresented in Table 13b.

                  TABLE 13b                                                       ______________________________________                                         ##STR738##                                                                                               Physical property values                          R.sup.b1    R.sup.b2                                                                              HZ      or characteristics                                ______________________________________                                        CH.sub.3    H       HI      m. p. 221-227° C.                          CH.sub.2 CHCH.sub.2                                                                       H       HBr     m. p. 131-132° C.                          CH.sub.2 CCH                                                                              H       HBr     m. p. 114-117° C.                          CH.sub.2 COCH.sub.3                                                                       H       HBr     m. p. 198-200° C.                          CH.sub.3    CH.sub.3                                                                              HI      m. p. 117-121° C.                          ______________________________________                                    

REFERENCE EXAMPLE c-1

Preparation of 2-imino-3-n-propoxythiazolidine hydrobromide ##STR739##

22 g (197 mmol) of n-propoxyamine hydrochloride was dissolved in 100 mlof water, and 200 ml of ethylene dichloride was added thereto. Then,27.2 g (197 mmol) of potassium carbonate was added in several timesunder cooling, and then 21.3 g (196 mmol) of ethyl chloroformate wasdropwise added thereto at a temperature of not higher than 10° C. Afterraising the temperature to room temperature, the mixture was furtherstirred at the same temperature for 4 hours. The ethylene dichloridelayer was separated, and then the aqueous layer was extracted twice with100 ml of chloroform. The ethylene dichloride layer and the chloroformlayer were put together, and washed with a saturated sodium chlorideaqueous solution, and then dried over anhydrous sodium sulfate. Then,the solvent was distilled off under reduced pressure. 27 g of ethylN-n-propoxycarbamate was obtained by distillation under reducedpressure.

Boiling point: 88° C./2.5 mmHg

8.73 g (218 mmol) of 60% sodium hydride was suspended in 200 ml of drytetrahydrofuran, and 50 ml of a dry tetrahydrofuran solution containing26.7 g (182 mmol) of ethyl N-n-propoxycarbamate, was dropwise addedthereto under cooling with ice at a temperature of not higher than 10°C. After raising the temperature to room temperature, the mixture wasstirred at the same temperature for 20 minutes and again cooled withice. Then, 121.4 g (646 mmol) of 1,2-dibromoethane was added all atonce. The temperature was gradually raised and then the mixture wasrefluxed under heating for 2 hours. The mixture was left to cool to roomtemperature, and the solvent was partially distilled off under reducedpressure. The residue was poured into 100 ml of ice water and extractedthree times with 100 ml of chloroform. The chloroform layer was washedwith a saturated sodium chloride aqueous solution and then dried overanhydrous sodium sulfate. The solvent was distilled off under reducedpressure, and then 42.0 g of ethyl N-(2-bromoethyl)-N-n-propoxycarbamatewas obtained by distillation under reduced pressure.

Boiling point: 97° C./0.4 mmHg

A mixture comprising 41.7 g (164 mmol) of ethylN-(2-bromoethyl)-N-n-propoxycarbamate, 16.2 g (213 mmol) of thiourea and200 ml of ethanol, was refluxed under heating for 5 hours. The mixturewas left to cool, and then the solvent was distilled off under reducedpressure. Then, 300 ml of chloroform was added to the residue, and themixture was stirred at room temperature for 10 minutes. After removinginsoluble matters by filtration, chloroform was distilled off underreduced pressure. To the residue, ethyl ether and a small amount ofwater were added for crystallization. Then, the crystals were collectedby filtration to obtain 50 g ofS-[2-(N-ethoxycarbonyl-N-n-propoxy)aminoethyl]isothiuroniumhydrobromide.

Melting point: 74°-76° C.

5.0 g (15.2 mmol) ofS-[2-(N-ethoxycarbonyl-N-n-propoxy)aminoethyl]isothiuronium hydrobromideand 0.27 g (15.0 mmol) of water were added to 30 ml of a 30% hydrogenbromide/acetic acid solution, and the mixture was heated and stirred at55° C. for 4 hours. The mixture was left to cool, and acetic acid wasdistilled off under reduced pressure. To the residue, ethyl ether and asmall amount of ethanol were added for crystallization. The crystalswere collected by filtration to obtain 3.8 g ofS-[2-(N-n-propoxy)aminoethyl]isothiuronium hydrobromide.

Melting point: 112°-113° C.

3.8 g (14.7 mmol) of S-[2-(N-n-propoxy)aminoethyl]isothiuroniumhydrobromide was added to 60 ml of ethanol, and the mixture was refluxedunder heating for 3 hours. The mixture was left to cool, and thenethanol was distilled off under reduced pressure. To the residue, ethylether and a small amount of ethanol were added for crystallization. Thecrystals were collected by filtration to obtain 3.2 g of2-imino-3-n-propoxythiazolidine hydrobromide.

Melting point: 117°-119° C.

REFERENCE EXAMPLE c-2

Preparation of 2-imino-3-methoxy-4-methylthiazol-4-ine hydrochloride##STR740##

5.67 g (70 mmol) of sodium thiocyanate was dissolved in 12 ml of water,and the solution was heated to 80° C. 5.55 g (60 mmol) of chloroacetonewas dropwise added thereto over a period of one hour, and the mixturewas stirred at the same temperature for 3 hours. The mixture was cooledto room temperature, and then 60 ml of ethyl ether was added thereto.The aqueous layer was separated and removed. The ethyl ether layer waswashed twice with 10 ml of water, and then the solvent was distilled offunder reduced pressure to obtain 6.0 g of thiocyanoacetone.

2.30 g (20 mmol) of thiocyanoacetone and 1.67 g (20 mmol) ofmethoxyamine hydrochloride were dissolved in 10 ml of ethanol, and thesolution was refluxed under heating for 5 hours. Ethanol was distilledoff under reduced pressure. Then, to the obtained residue, 50 ml ofethyl acetate was added. Precipitated crystals were collected byfiltration to obtain 3.34 g of 2-imino-3-methoxy-4-methylthiazol-4-inehydrochloride.

Melting point: 145°-155° C. (decomposed)

The structures and the physical property values of the compoundsprepared by the same methods as in Reference Examples c-1 and c-2 arepresented in Tables 13c-1, 13c-2 and 13c-3.

                  TABLE 13c-1                                                     ______________________________________                                         ##STR741##                                                                                                    Physical                                                                      property values                              R.sup.c1    R.sup.c2                                                                             R.sup.c3                                                                              HZ    or characteristics                           ______________________________________                                        C.sub.2 H.sub.5                                                                           H      H       HBr   m.p. 175-176° C.                      CH(CH.sub.3).sub.2                                                                        H      H       HBr   m.p. 150-152° C.                      CH.sub.3    H      H       HBr   Pale yellow glassy                           C.sub.4 H.sub.9 -n                                                                        H      H       HBr   m.p. 97-98° C.                        CH.sub.2 CCH                                                                              H      H       HBr   m.p. 139-140° C.                      CH.sub.2 CHCH.sub.2                                                                       H      H       HBr   m.p. 139-140° C.                      CH.sub.2 CHCHCl                                                                           H      H       HBr   m.p. 145-150° C.                      CH.sub.2 CH(CH.sub.3).sub.2                                                               H      H       HBr   m.p. 110-111° C.                      C.sub.5 H.sub.11 -n                                                                       H      H       HBr   Oil                                          CH.sub.2 C(Cl)CH.sub.2                                                                    H      H       HBr   m.p. 169-170° C.                      CH.sub.2 Ph H      H       HBr   m.p. 167-169° C.                      ______________________________________                                    

                  TABLE 13c-2                                                     ______________________________________                                         ##STR742##                                                                                                    Physical property values                     R.sup.c1                                                                            R.sup.c4                                                                              R.sup.c5                                                                              R.sup.c6                                                                           HZ    or characteristics                           ______________________________________                                        C.sub.2 H.sub.5                                                                     H       H       H    HBr   m.p. 209-210° C.                      ______________________________________                                    

                  TABLE 13c-3                                                     ______________________________________                                         ##STR743##                                                                                                 Physical property values                        R.sup.c1                                                                              R.sup.c7                                                                              R.sup.c8                                                                              HZ    or characteristics                              ______________________________________                                        CH.sub.3                                                                              CH.sub.3                                                                              CH.sub.3                                                                              HCl   m. p. 150-155° C.                                                      (decomposed)                                    ______________________________________                                    

REFERENCE EXAMPLE d-1

Preparation of 3-methyl-2-iminothiazolidin-4-one hydroiodide ##STR744##

11.6 g (0.1 mol) of pseudothiohydantoin was suspended in 150 ml ofdimethylformamide, and 17 g (0.12 mol) of methyl iodide was addedthereto. Then, the mixture was stirred at 60° C. for one hour. Afterbeing left to cool, the reaction mixture was poured into 1000 ml ofethyl acetate, and precipitated crystals were collected by filtration toobtain 15 g of 3-methyl-2-iminothiazolidin-4-one hydroiodide as paleyellow crystals.

Melting point: 237°-238° C.

REFERENCE EXAMPLE d-2

Preparation of 1-methyl-3-n-propyl-2-iminoimidazolidin-4-one hydroiodide##STR745##

9.04 g (80 mmol) of creatinine was suspended in 50 ml ofdimethylformamide, and 17.0 g (100 mmol) of n-propyl iodide was addedthereto. Then, the mixture was heated and stirred within a range of from70° C. to 80° C. until creatinine was completely dissolved. The mixturewas left to cool, and 500 ml of ethyl acetate was added thereto.Precipitated crystals were collected by filtration to obtain 10.6 g of1-methyl-3-n-propyl-2-iminoimidazolidin-4-one hydroiodide.

Melting point: 159°-161° C.

The 1-methyl-3-n-propyl-2-iminoimidazolidin-4-one hydroiodide wasneutralized in accordance with the following method to obtain1-methyl-3-n-propyl-2-iminoimidazolidin-4-one.

2.83 g (10 mmol) of the 1-methyl-3-n-propyl-2-iminoimidazolidin-4-onehydroiodide was added to 25 ml of methanol containing 0.66 g (10 mmol)of 85% potassium hydroxide, and the mixture was stirred at roomtemperature for one hour. Methanol was distilled off under reducedpressure, and chloroform was added to the residue. Precipitated crystalswere removed by filtration. Chloroform was distilled off under reducedpressure to obtain 1.16 g of 1-methyl-3-n-propyl-2-iminoimidazolidin-4-one as an oily substance.

The structures and the physical property values of the compoundsprepared by the same methods as in Reference Examples d-1 and d-2, arepresented in Table 13d.

                  TABLE 13d                                                       ______________________________________                                         ##STR746##                                                                                                  Physical property values                       R.sup.d1    R.sup.d4                                                                             R.sup.d5                                                                             HZ   or characteristics                             ______________________________________                                        CH.sub.3    H      CH.sub.3                                                                             HI   m.p. 215-216° C.                        C.sub.2 H.sub.5                                                                           H      CH.sub.3                                                                             HI   m.p. 220-222° C.                        CH.sub.2 CHCH.sub.2                                                                       H      CH.sub.3                                                                             HBr  m.p. 117-119° C.                        CH.sub.2 CCH                                                                              H      CH.sub.3                                                                             HBr  m.p. 228-230° C.                        CH.sub.2 COCH.sub.3                                                                       H      CH.sub.3                                                                             HBr  m.p. 188-190° C.                        CH.sub.2 CO.sub.2 CH.sub.3                                                                H      CH.sub.3                                                                             HBr  m.p. 201-203° C.                        CH.sub.2 OCH.sub.3                                                                        H      CH.sub.3                                                                             HCl  m.p. 198-199° C.                        CH.sub.2 SCH.sub.3                                                                        H      CH.sub.3                                                                             HCl  m.p. 200-210° C.                                                       (decomposed)                                   ______________________________________                                    

REFERENCE EXAMPLE e-1

Preparation of 3,6-dihydro-3-n-propyl-2H-1,3-thiazin-2-imine ##STR747##

1.3 g (11.4 mmol) of 2-amino-6H-1,3-thiazine was dissolved in 4 ml ofdimethylformamide, and 2.4 g (14.1 mmol) of n-propyl iodide was addedthereto. The mixture was heated at 50° C. for one hour and then stirredat room temperature overnight. To the reaction solution, 100 ml of ethylacetate was added, and the mixture was stirred and then left to standstill. Then, the ethyl acetate layer was separated and removed bydecantation. Then, the residual oily substance was dissolved in 50 ml ofmethanol, and 30 ml of a methanol solution containing 0.75 g (11.4 mmol)of 85% potassium hydroxide, was added thereto at room temperature. Themixture was further stirred at the same temperature for one hour, andthen methanol was distilled off under reduced pressure. To the residue,60 ml of chloroform was added, and insoluble matters were removed byfiltration. Then, the filtrate was concentrated under reduced pressure.The residual oily substance was purified by alumina columnchromatography (eluent: chloroform) to obtain 0.4 g of3,6-dihydro-3-n-propyl-2H-1,3-thiazin-2-imine as an oily substance.

REFERENCE EXAMPLE 2-e

Preparation of 3,4,5,6-tetrahydro-3-methyl-2H-1,3-thiazin-2-imine##STR748##

3.13 g (27 mmol) of 2-amino-4,5-dihydro-6H-1,3-thiazine was dissolved in20 ml of isopropyl alcohol, and 4.26 g (30 mmol) of methyl iodide wasadded thereto. The mixture was refluxed under heating for one hour, andthen left to cool. The solvent was distilled off under reduced pressure.Then, the residual oily substance was dissolved in 200 ml of methanol,and a 70 ml of a methanol solution containing 1.68 g (25.5 mmol) of 85%potassium hydroxide, was added thereto at room temperature. The mixturewas stirred at the same temperature for 5 minutes, and then methanol wasdistilled off under reduced pressure. To the residue, 300 ml ofchloroform was added and then dried over anhydrous sodium sulfate.Inorganic substances were removed by filtration, and then chloroform wasdistilled off under reduced pressure to obtain 3 g of3,4,5,6-tetrahydro-3-methyl-2H-1,3-thiazin-2-imine as a pale red oilysubstance.

The structures and the characteristics of the compounds prepared by thesame methods as in Reference Examples e-1 and e-2, are presented inTables 13e-1 and 13e-2.

                  TABLE 13e-1                                                     ______________________________________                                         ##STR749##                                                                                                  Physical property values                       R.sup.e1 R.sup.e2                                                                              R.sup.e3                                                                              R.sup.e4                                                                            or characteristics                             ______________________________________                                        CH.sub.3 H       H       H     Oil                                            CH.sub.2 OCH.sub.3                                                                     H       H       H     Oil                                            ______________________________________                                    

                  TABLE 13e-2                                                     ______________________________________                                         ##STR750##                                                                                                 Physical property values                        R.sup.e1                                                                              R.sup.e8                                                                              R.sup.e9                                                                              R.sup.e10                                                                           or characteristics                              ______________________________________                                        C.sub.3 H.sub.7 -n                                                                    H       H       H     Oil                                             ______________________________________                                    

REFERENCE EXAMPLE f-1

Preparation of 2-imino-3-methyloxazolidine hydroiodide ##STR751##

15 g (122 mmol) of 2-amino-2-oxazoline hydrochloride was stirred with8.4 g (128 mmol) of 85% potassium hydroxide in 400 ml of methanol atroom temperature for one hour. Methanol was distilled off under reducedpressure, and then 500 ml of chloroform was added. Precipitatedinsoluble substances were removed by filtration. Chloroform wasdistilled off under reduced pressure to obtain 10.5 g of2-amino-2-oxazoline.

Then, 10.5 g of 2-amino-2-oxazoline was dissolved in 40 ml ofdimethylformamide, and 22 g (155 mmol) of methyl iodide was addedthereto at room temperature. The mixture was further stirred at roomtemperature for 48 hours. Then, 1000 ml of ethyl acetate was added tothe reaction mixture. Formed crystals were collected by filtration,washed with ethyl acetate and then dried to obtain 23 g of2-imino-3-methyloxazolidine hydroiodide.

Melting point: 165°-169° C.

The structures and characteristics of the compounds prepared by the samemethod as in Reference Example f-1 are presented in Table 13f.

                  TABLE 13f                                                       ______________________________________                                         ##STR752##                                                                                                  Physical property values                       R.sup.f1  R.sup.f5                                                                              R.sup.f6                                                                             HZ    or characteristics                             ______________________________________                                        CH.sub.2 CHCH.sub.2                                                                     H       H      HBr   Glassy                                         ______________________________________                                    

REFERENCE EXAMPLE g-1

Preparation of N,N-dimethyl-S-methylisothiourea hydroiodide ##STR753##

35 g (0.5 mol) of N,N-dimethylcyanamide was dissolved in a mixedsolution of 70 ml of pyridine and 70 ml of triethylamine, and thesolution was heated to 60° C. Hydrogen sulfide gas was introducedthereinto for 30 minutes. Then, the reaction mixture was left to cool toroom temperature, and 300 ml of ethyl ether was added thereto.Precipitated crystals were collected by filtration and then washed withethyl ether to obtain 48 g of N,N-dimethylthiourea as pale browncrystals.

Melting point: 163°-164° C.

10.4 g (0.1 mol) of N,N-dimethylthiourea was suspended in 80 ml ofethanol, and 17 g (0.12 mol) of methyl iodide was added thereto. Themixture was refluxed under heating for 30 minutes. The reaction mixturewas left to cool to room temperature, and then the solvent was distilledoff under reduced pressure. The obtained crystals were washed with ethylether, collected by filtration and dried to obtain 20 g ofN,N-dimethyl-S-methylisothiourea hydroiodide as yellow crystals.

Melting point: 84°-85° C.

REFERENCE EXAMPLE g-2

Preparation of N-ethyl-N-methyl-S-methylisothiourea hydroiodide##STR754##

7.08 g (120 mmol) of N-ethyl-N-methylamine was dissolved in 80 ml of dryacetone, and the solution was cooled to 0° C. 13.1 g (100 mmol) ofethoxycarbonyl isothiocyanate was dropwise added thereto. Then, thereaction temperature was raised to room temperature, and the mixture wasfurther stirred at the same temperature for 2 hours. The solvent wasdistilled off under reduced pressure. To the obtained residue, 80 ml ofconcentrated hydrochloric acid was added. The reaction temperature wasraised to 80° C., and the mixture was further stirred at the sametemperature for 5 hours. Then, it was cooled to 0° C., and then ammoniumcarbonate was gradually added to neutralize the reaction mixture (pH=6to 7). After adding a small amount of water, the mixture was extractedthree times with 100 ml of ethyl acetate. The ethyl acetate layer waswashed with water and then dried over anhydrous sodium sulfate. Then,the solvent was distilled off under reduced pressure. Obtained crystalswere washed with a solvent mixture of ethanol/n-hexane to obtain 5.8 gof N-ethyl-N-methylthiourea as white crystals. Melting point: 124°-125°C.

5.8 g (49 mmol) of N-ethyl-N-methylthiourea was dissolved in 10 ml ofN,N-dimethylformamide. 8.8 g (62 mmol) of methyl iodide was added atroom temperature, and the mixture was stirred at room temperature for 15hours. 500 ml of ethyl acetate was added to the mixture, andprecipitated crystals were collected by filtration and then washed withethyl acetate to obtain 3.1 g of N-ethyl-N-methyl-S-methylisothioureahydroiodide as pale yellow crystals.

Melting point: 94°-97° C.

REFERENCE EXAMPLE g-3

Preparation of N-methoxy-N-methyl-S-methylisothiourea hydroiodide##STR755##

1.83 g (30 mmol) of N-methoxy-N-methylamine was dissolved in 20 ml ofdichloromethane, and the solution was cooled to 0° C. 3.93 g (30 mmol)of ethoxycarbonyl isothiocyanate was dropwise added thereto. Then, thereaction temperature was raised to room temperature, and the mixture wasfurther stirred at the same temperature for 15 hours. The solvent wasdistilled off under reduced pressure, and to the obtained residue, 20 mlof concentrated hydrochloric acid was added. The reaction temperaturewas raised to 80° C., and the mixture was further stirred at the sametemperature for 5 hours. Then, the mixture was cooled to 0° C., and thenammonium carbonate was gradually added to neutralize the reactionmixture (pH=6 to 7). After adding 10 ml of water, the mixture wasextracted three times with 50 ml of ethyl acetate. The ethyl acetatelayer was washed with water and then dried over anhydrous magnesiumsulfate. Then, the solvent was distilled off under reduced pressure toobtain 2.0 g of N-methoxy-N-methylthiourea as pale yellow crystals.Melting point: 30°-32° C.

1.76 g (14.7 mmol) of N-methoxy-N-methylthiourea was dissolved in 5 mlof N,N-dimethylformamide. 2.09 g (14.7 mmol) of methyl iodide was addedthereto at room temperature, and the mixture was stirred at roomtemperature for 15 hours. 500 ml of ethyl acetate was added thereto, andprecipitated crystals were collected by filtration and then washed withethyl acetate to obtain 2.7 g of N-methoxy-N-methyl-S-methylisothioureahydroiodide as pale yellow crystals.

Melting point: 122°-124° C.

The structures and physical property values or characteristics of thecompounds prepared by the same methods as in Reference Examples g-1 tog-3 are presented in Table 13g.

                  TABLE 13g                                                       ______________________________________                                         ##STR756##                                                                                                     Physical                                                                      property values                             R.sup.g1  R.sup.g2    R.sup.g3                                                                             HZ   or characteristics                          ______________________________________                                        C.sub.2 H.sub.5                                                                         CH.sub.3    CH.sub.3                                                                             HI   m. p. 93-94° C.                      C.sub.3 H.sub.7 -n                                                                      CH.sub.3    CH.sub.3                                                                             HI   m. p. 54-55° C.                      CH.sub.2 CHCH.sub.2                                                                     CH.sub.3    CH.sub.3                                                                             HBr  m. p. 148-149° C.                    CH.sub.2 CCH                                                                            CH.sub.3    CH.sub.3                                                                             HBr  m. p. 113-114° C.                    CH.sub.3  CH.sub.3 CO CH.sub.3                                                                             --   Glassy                                      CH.sub.3  (CH.sub.2).sub.4                                                                             HI     m. p. 121-123° C.                      CH.sub.3  C.sub.3 H.sub.7 -n                                                                        CH.sub.3                                                                             HI   m. p. 126-127° C.                    CH.sub.3  Ph          CH.sub.3                                                                             HI   m. p. 170-173° C.                    CH.sub.3  C.sub.2 H.sub.5 O                                                                         CH.sub.3                                                                             HI   m. p. 114-115° C.                    CH.sub.3  n-C.sub.3 H.sub.7 O                                                                       CH.sub.3                                                                             HI   m. p. 75-76° C.                      CH.sub.3  CH.sub.2 CHCH.sub.2                                                                       CH.sub.3                                                                             HI   m. p. 116-118° C.                    ______________________________________                                    

EXAMPLE a-1

Preparation of1-(3-methyl-4-thiazoline-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)urea##STR757##

1.55 g (10 mmol) of 2-amino-4,6-dimethoxypyrimidine was dissolved in 20ml of dry tetrahydrofuran, and 1.42 g (10 mmol) of chlorosulfonylisocyanate was dropwise added thereto within a range of from -10° C. to-5° C. The reaction temperature was raised to 0° C., and the mixture wasstirred for 5 minutes. The reaction mixture was again cooled to -30° C.,and 1.14 g (10 mmol) of 2-imino-3-methylthiazol-4-ine and 1.11 g (11mmol) of triethylamine dissolved in 10 ml of dry tetrahydrofuran weredropwise added thereto. The reaction temperature was raised to roomtemperature, and the mixture was further stirred at the same temperaturefor one hour. Then, the solvent was distilled off under reducedpressure. Then, water was added to the obtained residue. Precipitatedcrystals were collected by filtration and washed with acetonitrile toobtain 1.5 g of desired 1-(3-methyl-4-thiazoline-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)urea.

Melting point: 214°-215° C.

EXAMPLE a-2

Preparation of1-(3-n-propyl-4-thiazoline-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)urea##STR758##

1.55 g (10 mmol) of 2-amino-4,6-dimethoxypyrimidine was dissolved in 30ml of dry tetrahydrofuran, and 1.42 g (10 mmol) of chlorosulfonylisocyanate was dropwise added thereto at a temperature of not higherthan -20° C. The reaction temperature was raised to 0° C., and then themixture was cooled again to a temperature of not higher than -20° C.Then, 2.70 g (10 mmol) of 2-imino-3-n-propylthiazoyl-4-ine hydroiodideand 2.22 g (22 mmol) of triethylamine dissolved in 30 ml of drytetrahydrofuran were dropwise added thereto. The reaction temperaturewas raised to room temperature, and the mixture was further stirred atthe same temperature for one hour. Then, the solvent was distilled offunder reduced pressure. Then, water was added to the residue, and themixture was extracted three times with chloroform. The chloroform layerwas washed sequentially with water and a saturated sodium chlorideaqueous solution and then dried over anhydrous sodium sulfate. Then, thesolvent was distilled off under reduced pressure. The obtained crystalswere washed with ethyl ether to obtain 3 g of desired1-(3-n-propyl-4-thiazoline-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)urea.

Melting point: 166°-167° C.

EXAMPLE a-3

Preparation of1-(3-n-butylthiazolidine-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)urea##STR759##

1.55 g (10 mmol) of 2-amino-4,6-dimethoxypyrimidine was dissolved in 40ml of dry tetrahydrofuran, and 1.42 g (10 mmol) of chlorosulfonylisocyanate was dropwise added thereto at -40° C. The reactiontemperature was raised to 0° C., and then the reaction mixture wascooled again to -60° C. Then, 1.90 g (12 mmol) of2-imino-3-n-butylthiazolidine suspended in 40 ml of dry tetrahydrofurancontaining 1.33 g (13 mmol) of triethylamine, was added thereto. Thereaction temperature was raised to room temperature, and the mixture wasfurther stirred at the same temperature for one hour. Then, the solventwas distilled off under reduced pressure. Then, water was added to theresidue, and the mixture was extracted three times with chloroform. Thechloroform layer was washed sequentially with water and a saturatedsodium chloride aqueous solution, and then dried over anhydrous sodiumsulfate. Then, the solvent was distilled off under reduced pressure. Theobtained crystals were washed with ethyl ether to obtain 2.8 g ofdesired1-(3-n-butylthiazolidine-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)urea.

Melting point: 139°-140° C.

EXAMPLE a-4

Preparation of1-(1,3-dimethyl-4-imidazoline-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)urea##STR760##

540 mg (3.46 mmol) of 2-amino-4,6-dimethoxypyrimidine was dissolved in30 ml of dry tetrahydrofuran, and 490 mg (3.46 mmol) of chlorosulfonylisocyanate was dropwise added in a range of from -20° C. to -15° C. Thereaction temperature was raised to 0° C., and then the mixture wascooled again to -20° C. Then, a mixture comprising 600 mg (4.07 mmol) of2-imino-1,3-dimethylimidazol-4-ine hydrochloride, 820 mg (8.13 mmol) oftriethylamine and 30 ml of dry tetrahydrofuran, was added thereto. Thereaction temperature was raised to room temperature, and the mixture wasfurther stirred at the same temperature for 3 hours. Then, the solventwas distilled off under reduced pressure. Then, 60 ml of water was addedto the obtained residue, and crystals were collected by filtration. Theobtained crystals were washed with a solvent mixture of ethyl ether,acetonitrile and acetone to obtain 200 mg of desired1-(1,3-dimethyl-4-imidazoline-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)urea.

Melting point: 201°-203° C.

The structures and the physical property values of the compoundsprepared by the same methods as in Examples a-1 to a-4 are presented inTables 14a-1, 14a-2 and 14a-3.

                                      TABLE 14a-1                                 __________________________________________________________________________     ##STR761##                                                                   Compound                               m.p.                                   No.   R.sup.a1  R.sup.a2                                                                         R.sup.a3                                                                          L  A  B    D    (°C.)                           __________________________________________________________________________     4-a  CH.sub.2 CO.sub.2 CH.sub.3                                                              H  H   H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          166-167                                 5-a  CH.sub.2 Ph                                                                             H  H   H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          177-178                                 6-a  C.sub.2 H.sub.5                                                                         H  H   H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          189-190                                 7-a  CH.sub.2 CHCH.sub.2                                                                     H  H   H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          165-166                                 8-a  CH.sub.2 CCH                                                                            H  H   H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          183-184                                 9-a  CH.sub.2 CO.sub.2 C.sub.2 H.sub.5                                                       H  H   H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          137-138                                10-a  CH.sub.2 COCH.sub.3                                                                     H  H   H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          180-181                                11-a  CH(CH.sub.3)CO.sub.2 C.sub.2 H.sub.5                                                    H  H   H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          131-132                                12-a  C.sub.3 H.sub.7 -n                                                                      H  H   H  CH OCH.sub.3                                                                          CH.sub.3                                                                           167-170                                13-a  C.sub.3 H.sub.7 -n                                                                      H  H   H  CH CH.sub.3                                                                           CH.sub.3                                                                           155-158                                14-a  C.sub.3 H.sub.7 -n                                                                      H  H   H  CH OCHF.sub.2                                                                         OCHF.sub.2                                                                         152-154                                15-a  C.sub.3 H.sub.7 -n                                                                      H  H   H  CH OCHF.sub.2                                                                         CH.sub.3                                                                           143-145                                16-a  C.sub.3 H.sub.7 -n                                                                      H  H   H  N  OCH.sub.3                                                                          CH.sub.3                                                                           174-176                                17-a  CH.sub.3  CH.sub.3                                                                         H   H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          211-213                                18-a  CH.sub.3  CH.sub.3                                                                         CH.sub.3                                                                          H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          203-205                                19-a  C.sub.3 H.sub.7 -n                                                                      CH.sub.3                                                                         H   H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          176-178                                20-a  C.sub.4 H.sub.9 -n                                                                      H  H   H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          149-151                                21-a  C.sub.5 H.sub.11 -n                                                                     H  H   H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          160-161                                22-a  CH.sub.2 CHCHCH.sub.3                                                                   H  H   H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          123-125                                23-a  CH.sub.2 CHCHPh                                                                         H  H   H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          180-181                                27-a  CH.sub.2 CH.sub.2 OCH.sub.3                                                             H  H   H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          137.5-138.5                            28-a  C.sub.3 H.sub.7 -n                                                                      CH.sub.3                                                                         CH.sub.3                                                                          H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          199-201                                29-a  CH.sub.3  Ph H   H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          196-198                                30-a  CH.sub.3  H  Cl  H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          198-201                                31-a  CH.sub.3  H  Br  H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          209-211                                32-a  C.sub.3 H.sub.7 -n                                                                      H  Cl  H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          139-142                                33-a  CH.sub.2 OCH.sub.2 Ph                                                                   H  H   H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          168-169                                35-a  C.sub.6 H.sub.13 -n                                                                     H  H   H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          173-175                                36-a  CH.sub.2 CH(CH.sub.3).sub.2                                                             H  H   H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          177-179                                37-a  CH(CH.sub.3).sub.2                                                                      H  H   H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          175.5-176.5                            38-a  CH.sub.2 OCH.sub.3                                                                      H  H   H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          173-174                                39-a  CH(CH.sub.3)C.sub.2 H.sub.5                                                             H  H   H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          81-82                                  43-a  CH.sub.2 SCH.sub.3                                                                      H  H   H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          181-183                                44-a  CH.sub.2 CN                                                                             H  H   H  CH OCH.sub.3                                                                          OCH.sub.3                                                                            183-183.5                            45-a  CH.sub.2 C(Cl)CH.sub.2                                                                  H  H   H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          174-175                                46-a  C.sub.3 H.sub.7 -n                                                                      H  H   CH.sub.3                                                                         CH OCH.sub.3                                                                          OCH.sub.3                                                                          172-173                                47-a  C.sub.4 H.sub.9 -n                                                                      H  H   H  CH OCH.sub.3                                                                          CH.sub.3                                                                           147-149                                48-a  CH.sub.2 CHCHCl                                                                         H  H   H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          165-167                                49-a  CH.sub.2 C(CH.sub.3)CH.sub.2                                                            H  H   H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          177-179                                52-a  CH.sub.3  H  CH.sub.3                                                                          H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          206-208                                53-a  C.sub.3 H.sub.7 -n                                                                      H  CH.sub.3                                                                          H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          152-154                                54-a  CH.sub.3  H  OCH.sub.3                                                                         H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          187-190                                55-a  CH.sub.2 CHC(CH.sub.3).sub.2                                                            H  H   H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          170-171                                57-a  CH.sub.2 CH.sub.2 Ph                                                                    H  H   H  CH OCH.sub.2                                                                          OCH.sub.3                                                                          182-184                                58-a  CH.sub.2 PhOMeP                                                                         H  H   H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          109-110                                60-a  CH.sub.2 PhClP                                                                          H  H   H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          182-183                                61-a  CH.sub.2 C(Br)CH.sub.2                                                                  H  H   H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          167-168                                63-a  CH.sub.2 OC.sub.2 H.sub.5                                                               H  H   H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          177-178                                65-a  CH.sub.2 CCCH.sub.3                                                                     H  H   H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          184-186                                68-a  C.sub.3 H.sub.7 -n                                                                      H  H   H  CH OCH.sub.3                                                                          Cl   165-168                                72-a  C.sub.3 H.sub.7 -n                                                                      H  H   H  CH OCH.sub.3                                                                          OCHF.sub.2                                                                         193-195                                73-a  C.sub.3 H.sub.7 -n                                                                      H  H   H  N  OCH.sub.3                                                                          OCH.sub.3                                                                          156-158                                79-a  C.sub.3 H.sub.7 -n                                                                      H  H   H  N  OC.sub.2 H.sub.5                                                                   CH.sub.3                                                                           151-153                                80-a  C.sub.3 H.sub.7 -n                                                                      H  H   H  N  OCH.sub. 3                                                                         C.sub.2 H.sub.5                                                                    141-143                                82-a  C.sub.3 H.sub.7 -n                                                                      H  H   H  N  OCH.sub.3                                                                          CH.sub.2 Cl                                                                        144-146                                83-a  C.sub.3 H.sub.7 -n                                                                      H  H   H  CH CF.sub.3                                                                           Cl   146-148                                84-a  C.sub.3 H.sub.7 -n                                                                      H  H   H  N  OCH.sub.3                                                                          C.sub.3 H.sub.7 -n                                                                 159-160                                85-a  C.sub.3 H.sub.7 -n                                                                      H  H   H  N  OCH.sub.3                                                                          CF.sub.3                                                                           149-150                                86-a  C.sub.3 H.sub.7 -n                                                                      H  H   H  N  OC.sub.3 H.sub.7 -n                                                                CH.sub.3                                                                           176-178                                __________________________________________________________________________

                                      TABLE 14a-2                                 __________________________________________________________________________     ##STR762##                                                                   Compound                           m.p.                                       No.   R.sup.a1  R.sup.a4                                                                         R.sup.a5                                                                         A  B    D    (°C.)                               __________________________________________________________________________     3-a  CH.sub.3  H  H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          204-206                                    24-a  C.sub.3 H.sub.7 -n                                                                      H  H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          172-173                                    25-a  CH.sub.2 CHCH.sub.2                                                                     H  H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          177-178                                    26-a  CH.sub.2 CCH                                                                            H  H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          188-190                                    34-a  C.sub.2 H.sub.5                                                                         H  H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          170-172                                    41-a  CH.sub.2 CHCHCH.sub.3                                                                   H  H  CH OCH.sub.3                                                                          OCHS 133-134                                    42-a  C.sub.5 H.sub.11 -n                                                                     H  H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          132-134                                    50-a  CH.sub.2 COCH.sub.3                                                                     H  H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          186-188                                    51-a  C.sub.6 H.sub.13 -n                                                                     H  H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          163-165                                    56-a  CH.sub.3  H  CH.sub.3                                                                         CH OCH.sub.3                                                                          OCH.sub.3                                                                          190-191                                    59-a  CH.sub.2 CHCHCl                                                                         H  H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          155-156                                    62-a  CH.sub.2 C(Cl)CH.sub.2                                                                  H  H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          190-191                                    64-a  CH.sub.2 OCH.sub.3                                                                      H  H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          169-170                                    70-a  C.sub.3 H.sub.7 -n                                                                      H  H  CH OCH.sub.3                                                                          Cl   144-146                                    71-a  C.sub.3 H.sub.7 -n                                                                      H  H  CH OCH.sub.3                                                                          OCHF.sub.2                                                                         144-145                                    74-a  C.sub.3 H.sub.7 -n                                                                      H  H  CH OCH.sub.3                                                                          CH.sub.3                                                                           175-177                                    75-a  C.sub.3 H.sub.7 -n                                                                      H  H  CH CH.sub.3                                                                           CH.sub.3                                                                           166-168                                    76-a  C.sub.3 H.sub.7 -n                                                                      H  H  CH OCHF.sub.2                                                                         OCHF.sub.2                                                                         173-174                                    77-a  C.sub.3 H.sub.7 -n                                                                      H  H  CH CH.sub.3                                                                           Cl   155-158                                    78-a  C.sub.3 H.sub.7 -n                                                                      H  H  N  OCH.sub.3                                                                          CH.sub.3                                                                           184-186                                    81-a  Ph        H  H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          178-180                                    __________________________________________________________________________

                  TABLE 14a-3                                                     ______________________________________                                         ##STR763##                                                                   Com-                                                                          pound                                           m.p.                          No.   R.sup.a1                                                                              R.sup.a2                                                                             R.sup.a3                                                                           R.sup.a6                                                                           A    B     D     (°C.)                  ______________________________________                                        67-a  C.sub.2 H.sub.5                                                                       H      H    CH.sub.3                                                                           CH   OCH.sub.3                                                                           OCH.sub.3                                                                           178-                                                                          180                           69-a  C.sub.3 H.sub.7 -n                                                                    H      H    CH.sub.3                                                                           CH   OCH.sub.3                                                                           OCH.sub.3                                                                           167-                                                                          169                           ______________________________________                                    

EXAMPLE b-1

Preparation of1-(3-n-propyl-4-thiadiazoline-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)urea##STR764##

1.55 g (10 mmol) of 2-amino-4,6-dimethoxypyrimidine was dissolved in 40ml of dry tetrahydrofuran, and 1.42 g (10 mmol) of chlorosulfonylisocyanate was dropwise added at -40° C. The reaction temperature wasraised to 0° C., and then the mixture was cooled again to -40° C. Then,2.58 g (9.5 mmol) of 2-imino-3-n-propylthiadiazol-4-ine hydroiodidesuspended in 40 ml of dry tetrahydrofuran containing 2.22 g (22 mmol) oftriethylamine, was added thereto. The reaction temperature was raised toroom temperature, and the mixture was further stirred at the sametemperature for one hour. Then, the solvent was distilled off underreduced pressure, and then water was added to the obtained residue. Themixture was extracted three times with chloroform. The chloroform layerwas washed sequentially with water and a saturated sodium chlorideaqueous solution and then dried over anhydrous sodium sulfate. Then, thesolvent was distilled off under reduced pressure. Obtained crystals werewashed with acetonitrile to obtain 2.25 g of desired1-(3-n-propyl-4-thiadiazoline-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)urea.

Melting point: 189°-190° C.

The structures and the physical property values of the compoundsprepared by the same method as in Example b-1 are presented in Table14b.

                  TABLE 14b                                                       ______________________________________                                         ##STR765##                                                                   Com-                                                                          pound                                     m.p.                                No.   R.sup.b1    R.sup.b2                                                                             A    B     D     (°C.)                        ______________________________________                                        2-b   CH.sub.3    H      CH   OCH.sub.3                                                                           OCH.sub.3                                                                           216-217                             3-b   CH.sub.2 CHCH.sub.2                                                                       H      CH   OCH.sub.3                                                                           OCH.sub.3                                                                           197-198                             4-b   CH.sub.2 CCH                                                                              H      CH   OCH.sub.3                                                                           OCH.sub.3                                                                           196-198                             5-b   CH.sub.2 COCH.sub.3                                                                       H      CH   OCH.sub.3                                                                           OCH.sub.3                                                                           206-208                             6-b   CH.sub.3    CH.sub.3                                                                             CH   OCH.sub.3                                                                           OCH.sub.3                                                                           203.5-                                                                        204.5                               ______________________________________                                    

EXAMPLE c-1

Preparation of1-(3-ethoxythiazolidine-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)urea##STR766##

1.55 g (10 mmol) of 2-amino-4,6-dimethoxypyrimidine was dissolved in 20ml of dry tetrahydrofuran, and 1.42 g (10 mmol) of chlorosulfonylisocyanate was dropwise added thereto in a range of -10° C. to -5° C.The reaction temperature was raised to 0° C., and the mixture wasstirred for 5 minutes. The reaction mixture was cooled again to -30° C.,and 2.72 g (12 mmol) of 2-imino-3-ethoxythiazolidine hydrobromide and2.43 g (24 mmol) of triethylamine suspended in 10 ml of drytetrahydrofuran were gradually added thereto. The reaction temperaturewas raised to room temperature, and the mixture was further stirred atthe same temperature for 20 minutes. Then, the solvent was distilled offunder reduced pressure, and then water was added to the obtainedresidue. Precipitated crystals were extracted three times with 100 ml ofchloroform, and the extract was washed once with 100 ml of water anddried over anhydrous sodium sulfate. Then, the solvent was distilled offunder reduced pressure. Obtained crystals were washed with ethyl etherand acetonitrile to obtain 2.1 g of desired1-(3-ethoxythiazolidine-2-sulfonylimino)-3-(4,6-dimethoxypyridimin-2-yl)urea.

Melting point: 175°-176° C.

EXAMPLE c-2

Preparation of1-(3-n-propoxythiazolidine-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)urea##STR767##

0.62 g (4.0 mmol) of 2-amino-4,6-dimethoxypyrimidine was dissolved in 30ml of dry tetrahydrofuran, and 0.57 g (4.0 mmol) of chlorosulfonylisocyanate was dropwise added at -50° C. The reaction temperature wasraised to room temperature, and then the reaction mixture was cooledagain to -50° C. Then, 1.2 g (5.0 mmol) of2-imino-3-n-propoxythiazolidine hydrobromide suspended in 20 ml of drytetrahydrofuran containing 1.01 g (10.0 mmol) of triethylamine, wasadded thereto. The reaction temperature was gradually raised to roomtemperature, and the mixture was further stirred at the same temperaturefor 10 minutes. Then, the solvent was distilled off under reducedpressure, and then water was added to the obtained residue. The mixturewas extracted three times with 50 ml of chloroform. The chloroform layerwas washed with a saturated sodium chloride aqueous solution and thendried over anhydrous sodium sulfate. Then, the solvent was distilled offunder reduced pressure. To the obtained residue, ethyl ether and a smallamount of acetonitrile were added for crystallization. The crystals werecollected by filtration to obtain 0.65 g of desired1-(3-n-propoxythiazolidine-2-sulfonylimino)-3-(4,6-dimethoxypyridimin-2-yl)urea.

Melting point: 173°-175° C.

EXAMPLE c-3

Preparation of1-(3-n-propoxythiazolidine-2-sulfonylimino)-3-(4,6-dimethoxytriazin-2-yl)urea##STR768##

3.76 g (40.0 mmol) of phenol was dissolved in 40 ml of drytetrahydrofuran, and 5.66 g (40.0 mmol) of chlorosulfonyl isocyanate wasdropwise added thereto at -50° C. The reaction temperature was raised toroom temperature, and then the reaction mixture was cooled again to -50°C. Then, 10.6 g (44 mmol) of 2-imino-3-n-propoxythiazolidinehydrobromide suspended in 20 ml of dry acetonitrile containing 8.08 g(80 mmol) of triethylamine, was added thereto. The reaction temperaturewas gradually raised to room temperature, and the mixture was furtherstirred at the same temperature for 10 minutes. Then, the solvent wasdistilled off under reduced pressure, and then water was added to theobtained residue. The mixture was extracted three times with 70 ml ofchloroform. The chloroform layer was washed with a saturated sodiumchloride aqueous solution and then dried over anhydrous sodium sulfate.Then, the solvent was distilled off under reduced pressure. To theobtained residue, ethyl ether and a small amount of acetonitrile wereadded for crystallization. Then, the crystals were collected byfiltration to obtain 14 g of phenyl N-(3-n-propoxythiazolidine-2-sulfonylimino)carbamate. Then, 0.72 g (2.0 mmol) of the obtainedcarbamate was dissolved in 30 ml of dry dioxane, and 0.23 g (1.5 mmol)of 2-amino-4,6-dimethoxytriazine was added thereto. The mixture wasrefluxed under heating for 4 hours. The solvent was distilled off underreduced pressure, and ethyl ether and a small amount of acetonitrilewere added for crystallization. Then, the crystals were collected byfiltration to obtain 0.3 g of desired1-(3-n-propoxythiazolidine-2-sulfonylimino)-3-(4,6-dimethoxytriazin-2-yl)urea.

Melting point: 166°-167° C.

EXAMPLE c-4

Preparation of1-[3-(3-chloroallyloxy)thiazolidine-2-sulfonylimino]-3-(4-methyl-6-methoxytriazin-2-yl)urea##STR769##

0.84 g (6 mmol) of 2-amino-4-methyl-6-methoxytriazine was suspended in20 ml of dry tetrahydrofuran, and 0.85 g (6 mmol) of chlorosulfonylisocyanate was dropwise added thereto at room temperature. A heat wasgenerated mildly, and the reaction mixture turned to a pale yellowsolution. Then, 1.64 g (6 mmol) of2-imino-3-(3-chloroallyloxy)thiazolidine hydrobromide and 1.43 g (14mmol) of triethylamine suspended in 15 ml of dry tetrahydrofuran weregradually added thereto, and the mixture was further stirred at roomtemperature for 30 minutes. The solvent was distilled off under reducedpressure, and then water was added to the obtained residue. Theresulting oily substance was extracted three times with 80 ml ofchloroform. The extract solution was washed once with 100 ml of waterand dried over anhydrous sodium sulfate. Then, the solvent was distilledoff under reduced pressure. Obtained crystals were washed with ethylether and acetonitrile to obtain 1.2 g of desired1-[3-(3-chloroallyloxy)thiazolidine-2-sulfonylimino]-3-(4-methyl-6-methoxytriazin-2-yl)urea.

Melting point: 145°-147° C.

EXAMPLE c-5

Preparation of1-(3-methoxy-4-methyl-4-thiazoline-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)urea##STR770##

0.78 g (5 mmol) of 2-amino-4,6-dimethoxypyrimidine was dissolved in 10ml of dry tetrahydrofuran, and 0.71 g (5 mmol) of chlorosulfonylisocyanate was dropwise added thereto in a range of -20° C. to -15° C.The reaction temperature was raised to 0° C., and the mixture wasstirred for 5 minutes. The mixture was cooled again to -20° C., and 0.90g (5 mmol) of 2-imino-3-methoxy-4-methylthiazol-4-ine hydrochloride and1.11 g (11 mmol) of triethylamine suspended in 10 ml of drytetrahydrofuran, was gradually added thereto. The reaction temperaturewas raised to room temperature, and the mixture was further stirred atthe same temperature for 20 minutes. The solvent was distilled off underreduced pressure, and then water was added to the obtained residue.Precipitated crystals were extracted three times with 50 ml ofchloroform. The extract solution was washed once with 50 ml of water anddried over anhydrous sodium sulfate. Then, the solvent was distilled offunder reduced pressure. Obtained crystals were washed with ethyl etherand acetonitrile to obtain 1.02 g of desired1-(3-methoxy-4-methyl-4-thiazolidine-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)urea.

Melting point: 183°-185° C.

The structures and the physical property values of the compoundsprepared by the same methods as in Examples c-1 to c-5 are presented inTables 14c-1, 14c-2 and 14c-3.

                                      TABLE 14c-1                                 __________________________________________________________________________     ##STR771##                                                                   Compound                          m.p.                                        No.   R.sup.c1 R.sup.c2                                                                         R.sup.c3                                                                         A  B    D    (°C.)                                __________________________________________________________________________     2-c  C.sub.2 H.sub.5                                                                        H  H  CH OCH.sub.3                                                                          CH.sub.3                                                                           182-183                                      3-c  C.sub.2 H.sub.5                                                                        H  H  N  OCH.sub.3                                                                          CH.sub.3                                                                           155-156                                      4-c  C.sub.2 H.sub.5                                                                        H  H  CH CH.sub.3                                                                           CH.sub.3                                                                           152-153                                      5-c  CH(CH.sub.3).sub.2                                                                     H  H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          175-178                                      6-c  CH.sub.3 H  H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          193-194                                      7-c  CH.sub.3 H  H  CH OCH.sub.3                                                                          CH.sub.3                                                                           183-185                                     11-c  CH(CH.sub.3 ).sub.2                                                                    H  H  CH OCH.sub.3                                                                          CH.sub.3                                                                           150-152                                     13-c  C.sub.3 H.sub.7 -n                                                                     H  H  CH OCH.sub.3                                                                          CH.sub.3                                                                           161.5-162.5                                 14-c  C.sub.3 H.sub.7 -n                                                                     H  H  N  OCH.sub.3                                                                          CH.sub.3                                                                           163-165                                     15-c  C.sub.3 H.sub.7 -n                                                                     H  H  CH CH.sub.3                                                                           CH.sub.3                                                                           145.5-146.5                                 16-c  C.sub.4 H.sub.9 -n                                                                     H  H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          159-160                                     17-c  CH.sub.2 CCH                                                                           H  H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          172-173                                     18-c  CH.sub.2 CHCH.sub.2                                                                    H  H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          175.5-176.5                                 19-c  CH.sub.2 CHCH.sub.2                                                                    H  H  CH OCH.sub.3                                                                          CH.sub.3                                                                           165-166                                     20-c  C.sub.3 H.sub.7 -n                                                                     H  H  CH OCHF.sub.2                                                                         OCHF.sub.2                                                                         118-119                                     21-c  CH.sub.2 CHCH.sub.2                                                                    H  H  CH CH.sub.3                                                                           CH.sub.3                                                                           95-96                                       22-c  CH.sub.2 Ph                                                                            H  H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          159-161                                     23-c  C.sub.3 H.sub.7 -n                                                                     H  H  CH OCHF.sub.2                                                                         CH.sub.3                                                                           151-152                                     25-c  C.sub.3 H.sub.7 -n                                                                     H  H  CH OCHF.sub.2                                                                         Cl   225-226                                     26-c  C.sub.2 H.sub.5                                                                        H  H  N  OCH.sub.3                                                                          OCH.sub.3                                                                          159-160                                     27-c  C.sub.2 H.sub.5                                                                        H  H  CH OCHF.sub.2                                                                         CH.sub.3                                                                           148-149                                     28-c  C.sub.2 H.sub.5                                                                        H  H  CH OCHF.sub.2                                                                         OCHF.sub.2                                                                         161-162                                     29-c  C.sub.3 H.sub.7 -n                                                                     H  H  CH OCH.sub.3                                                                          OCHF.sub.2                                                                         75-77                                       30-c  C.sub.2 H.sub.5                                                                        H  H  CH OCH.sub.3                                                                          OCHF.sub.2                                                                         149-151                                     31-c  C.sub.2 H.sub.5                                                                        H  H  CH OCH.sub.3                                                                          Cl   141-143                                     32-c  C.sub.3 H.sub.7 -n                                                                     H  H  CH OCH.sub.3                                                                          Cl   157-158                                     33-c  C.sub.2 H.sub.5                                                                        H  H  CH CH.sub.3                                                                           Cl   163-164                                     34-c  C.sub.3 H.sub.7 -n                                                                     H  H  CH CH.sub.3                                                                           Cl   153-156                                     35-c  CH.sub.2 CHCHCl                                                                        H  H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          184-185                                     36-c  CH.sub.2 CHCHCl                                                                        H  H  CH OCH.sub.3                                                                          CH.sub.3                                                                           168-169                                     38-c  CH.sub.2 CH(CH.sub.3).sub.2                                                            H  H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          175.5-176.5                                 39-c  CH.sub.2 CH(CH.sub.3).sub.2                                                            H  H  CH OCH.sub.3                                                                          CH.sub.3                                                                           151-152                                     40-c  CH.sub.2 CH(CH.sub.3).sub.2                                                            H  H  N  OCH.sub.3                                                                          CH.sub.3                                                                           148.5-149.5                                 41-c  CH.sub. 2 CH(CH.sub.3).sub.2                                                           H  H  N  OCH.sub.3                                                                          OCH.sub.3                                                                          172-173                                     43-c  CH.sub.2 CHCHCl                                                                        H  H  CH CH.sub.3                                                                           CH.sub.3                                                                           164-165                                     44-c  CH.sub.2 CHCHCl                                                                        H  H  N  OCH.sub.3                                                                          OCH.sub.3                                                                          158-163                                     46-c  C.sub.5 H.sub.11 -n                                                                    H  H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          121-122                                     47-c  CH.sub.2 CH(CH.sub.3).sub.2                                                            H  H  CH CH.sub.3                                                                           CH.sub.3                                                                           154-155                                     48-c  CH.sub.2 CHCHCl                                                                        H  H  CH OCH.sub.3                                                                          OCHF.sub.2                                                                         142-143                                     49-c  CH.sub.2 C(Cl)CH.sub.2                                                                 H  H  CH OCH.sub.3                                                                          OCH.sub.3                                                                          178-179                                     50-c  CH.sub.2 C(Cl)CH.sub.2                                                                 H  H  CH OCH.sub.3                                                                          CH.sub.3                                                                           159-160                                     51-c  CH.sub.2 C(Cl)CH.sub.2                                                                 H  H  N  OCH.sub.3                                                                          CH.sub.3                                                                           157-158                                     52-c  CH.sub.2 C(Cl)CH.sub.2                                                                 H  H  N  OCH.sub.3                                                                          OCH.sub.3                                                                          181-182                                     53-c  C.sub.3 H.sub.7 -n                                                                     H  H  N  OC.sub.2 H.sub.5                                                                   CH.sub.3                                                                           134-135                                     54-c  C.sub.3 H.sub.7 -n                                                                     H  H  N  OCH.sub.3                                                                          C.sub.2 H.sub.5                                                                    143.5-144.5                                 55-c  CH.sub.2 CHCHCl                                                                        H  H  N  OC.sub.2 H.sub.5                                                                   CH.sub.3                                                                           131-133                                     56-c  CH.sub.2 CHCHCl                                                                        H  H  N  OCH.sub.3                                                                          C.sub.2 H.sub.5                                                                    128-130                                     57-c  CH.sub.2 CHCHCl                                                                        H  H  N  OCH.sub.3                                                                          CH.sub.2 Cl                                                                        133-135                                     58-c  C.sub.3 H.sub.7 -n                                                                     H  H  N  OCH.sub.3                                                                          CH.sub.2 Cl                                                                        154-155                                     59-c  CH.sub.2 CHCHCl                                                                        H  H  CH OCHF.sub.2                                                                         CH.sub.3                                                                           136-137                                     60-c  C.sub.3 H.sub.7 -n                                                                     H  H  CH CF.sub.3                                                                           Cl   133-134                                     61-c  C.sub.2 H.sub.5                                                                        H  H  N  OC.sub.2 H.sub.5                                                                   CH.sub.3                                                                           161-162                                     62-c  C.sub.3 H.sub.7 -n                                                                     H  H  N  OCH.sub.3                                                                          C.sub.3 H.sub.7 -n                                                                 157-158                                     63-c  C.sub.3 H.sub.7 -n                                                                     H  H  N  OC.sub.3 H.sub.7 -n                                                                CH.sub.3                                                                           124-125                                     64-c  CH.sub.2 CHCHCl                                                                        H  H  CH CF.sub.3                                                                           Cl   183-186                                     65-c  CH.sub.2 CHCHCl                                                                        H  H  N  OCH.sub.3                                                                          C.sub.3 H.sub.7 -n                                                                 114-115                                     66-c  CH.sub.2 CHCHCl                                                                        H  H  N  OC.sub.3 H.sub.7 -n                                                                CH.sub.3                                                                           128-130                                     67-c  CH.sub.2 CHCHCl                                                                        H  H  N  OCH.sub.3                                                                          CF.sub.3                                                                           138-140                                     68-c  CH.sub.2 C(Cl)CH.sub.2                                                                 H  H  N  OC.sub.2 H.sub.5                                                                   CH.sub.3                                                                           139-140                                     69-c  CH.sub.2 C(Cl)CH.sub.2                                                                 H  H  N  OCH.sub.3                                                                          C.sub.2 H.sub.5                                                                    149-150                                     70-c  CH.sub.2 C(Cl)CH.sub.2                                                                 H  H  N  OCH.sub.3                                                                          CF.sub.3                                                                           152-154                                     71-c  CH.sub.2 C(Cl)CH.sub.2                                                                 H  H  CH OCH.sub.3                                                                          OCHF.sub.2                                                                         86-87                                       __________________________________________________________________________

                                      TABLE 14c-2                                 __________________________________________________________________________     ##STR772##                                                                   Compound                        m.p.                                          No.   R.sup.c1                                                                          R.sup.c4                                                                         R.sup.c5                                                                          R.sup.c6                                                                         A  B    D   (°C.)                                  __________________________________________________________________________    8-c   C.sub.2 H.sub.5                                                                   H  H   H  CH OCH.sub.3                                                                          OCH.sub.3                                                                         189-190                                       9-c   C.sub.2 H.sub.5                                                                   H  H   H  CH OCH.sub.3                                                                          CH.sub.3                                                                          165-166                                       10-c  C.sub.2 H.sub.5                                                                   H  H   H  CH CH.sub.3                                                                           CH.sub.3                                                                          178-179                                       __________________________________________________________________________

                  TABLE 14c-3                                                     ______________________________________                                         ##STR773##                                                                   Com-                                                                          pound                                     m.p.                                No.   R.sup.c1                                                                             R.sup.c7                                                                             R.sup.c8                                                                           A    B     D     (°C.)                        ______________________________________                                        42-c  CH.sub.3                                                                             CH.sub.3                                                                             CH.sub.3                                                                           CH   OCH.sub.3                                                                           OCH.sub.3                                                                           180-192                                                                       (decomposed)                        ______________________________________                                    

EXAMPLE d-1

Preparation of1-(3-methylthiazolidin-4-one-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)urea##STR774##

1.55 g (10 mmol) of 2-amino-4,6-dimethoxypyrimidine was dissolved in 30ml of dry tetrahydrofuran, and 1.42 g (10 mmol) of chlorosulfonylisocyanate was dropwise added thereto in a range of from -20° C. to -15°C. The reaction temperature was raised to 0° C., and the mixture wasfurther stirred at the same temperature for 10 minutes. The reactionmixture was cooled again to -30° C., and a mixture comprising 2.84 g (11mmol) of 3-methyl-2-iminothiazolidin-4-one hydroiodide, 2.22 g (22 mmol)of triethylamine and 30 ml of dry tetrahydrofuran, was added thereto.The reaction temperature was raised to room temperature, and the mixturewas further stirred at the same temperature for 20 minutes. Then, thesolvent was distilled off under reduced pressure, and then 100 ml ofwater was added to the obtained residue. Precipitated crystals wereextracted three times with 100 ml of chloroform. The chloroform layerwas washed with water and then dried over anhydrous sodium sulfate.Then, the solvent was distilled off under reduced pressure. Obtainedcrystals were washed with a solvent mixture of ethyl ether/acetonitrileand collected by filtration to obtain 1.5 g of desired1-(3-methylthiazolidin-4-one-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)ureaas colorless crystals.

Melting point: 200°-201° C.

EXAMPLE d-2

Preparation of1-(1-methyl-3-n-propylimidazolidin-4-one-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)urea##STR775##

1.16 g (7.5 mmol) of 2-amino-4,6-dimethoxypyrimidine was dissolved in 20ml of dry tetrahydrofuran, and 1.07 g (7.5 mmol) of chlorosulfonylisocyanate was dropwise added thereto at -40° C. The reactiontemperature was raised to 0° C., and then the reaction mixture wascooled again to -40° C. Then, a mixture comprising 1.16 g (7.5 mmol) of1-methyl-3-n-propyl-2-iminoimidazolidin-4-one, 0.83 g (8.2 mmol) oftriethylamine and 20 ml of dry tetrahydrofuran, was added thereto. Thereaction temperature was raised to room temperature, and the mixture wasfurther stirred at the same temperature for 2 hours. Then, the solventwas distilled off under reduced pressure, and then 100 ml of water wasadded to the obtained residue. The mixture was extracted three timeswith 100 ml of chloroform. Then, the chloroform layer was washed withwater and then dried over anhydrous sodium sulfate. The solvent wasdistilled off under reduced pressure, and precipitated crystals werewashed with a solvent mixture of ethyl ether/acetonitrile and collectedby filtration to obtain 0.16 g of desired1-(1-methyl-3-n-propylimidazolidin-4-one-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)urea.

Melting point: 96°-98° C.

The structures and the physical property values of the compoundsprepared by the same methods as in Examples d-1 and d-2 are presented inTable 14d.

                                      TABLE 14d                                   __________________________________________________________________________     ##STR776##                                                                   Compound                       m.p.                                           No.   R.sup.d1                                                                              R.sup.d4                                                                         R.sup.d5                                                                         A  B   D   (°C.)                                   __________________________________________________________________________    3-d   CH.sub.3                                                                              H  CH.sub.3                                                                         CH OCH.sub.3                                                                         OCH.sub.3                                                                         188-189                                        4-d   C.sub.2 H.sub.5                                                                       H  CH.sub.3                                                                         CH OCH.sub.3                                                                         OCH.sub.3                                                                         111-113                                        5-d   CH.sub.2 CHCH.sub.2                                                                   H  CH.sub.3                                                                         CH OCH.sub.3                                                                         OCH.sub.3                                                                         156-158                                        6-d   CH.sub.2 CCH                                                                          H  CH.sub.3                                                                         CH OCH.sub.3                                                                         OCH.sub.3                                                                         181-182                                        7-d   CH.sub.2 COCH.sub.3                                                                   H  CH.sub.3                                                                         CH OCH.sub.3                                                                         OCH.sub.3                                                                         190-192                                        8-d   CH.sub.2 CO.sub. 2 CH.sub.3                                                           H  CH.sub.3                                                                         CH OCH.sub.3                                                                         OCH.sub.3                                                                         188-190                                        9-d   CH.sub.2 OCH.sub.3                                                                    H  CH.sub.3                                                                         CH OCH.sub.3                                                                         OCH.sub.3                                                                         155-156                                        10-d  CH.sub.2 SCH.sub.3                                                                    H  CH.sub.3                                                                         CH OCH.sub.3                                                                         OCH.sub.3                                                                         115-120                                                                       (decomposed)                                   __________________________________________________________________________

EXAMPLE e-1

Preparation of1-(3,6-dihydro-3-n-propyl-2H-1,3-thiazine-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)urea##STR777##

0.32 g (2.06 mmol) of 2-amino-4,6-dimethoxypyrimidine was dissolved in40 ml of dry tetrahydrofuran, and the solution was cooled to -40° C. Atthe same temperature, 0.29 g (2.05 mmol) of chlorosulfonyl isocyanatewas dropwise added thereto. Then, the temperature was raised to 0° C.The mixture was cooled again to -40° C., and then a mixed solutioncomprising 0.4 g (2.56 mmol) of3,6-dihydro-3-n-propyl-2H-1,3-thiazin-2-imine, 0.26 g (2.57 mmol) oftriethylamine and 40 ml of dry tetrahydrofuran, was dropwise addedthereto. The mixture was gradually heated to room temperature withstirring, and then the solvent was distilled off under reduced pressure.100 ml of water was added to the residue, and then the mixture wasextracted twice with 50 ml of chloroform. The chloroform layer waswashed with water and then dried over anhydrous sodium sulfate. Then,chloroform was distilled off under reduced pressure. Obtained crystalswere washed with acetonitrile and then with ethyl ether to obtain 0.3 gof desired 1-(3,6-dihydro-3-n-propyl-2H-1,3-thiazine-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl) urea.

Melting point: 161°-163° C.

EXAMPLE e-2

Preparation of1-(3,4,5,6-tetrahydro-3-methyl-2H-1,3-thiazine-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2yl)urea##STR778##

1.55 g (10 mmol) of 2-amino-4,6-dimethoxypyrimidine was dissolved in 30ml of dry tetrahydrofuran, and 1.42 g (10 mmol) of chlorosulfonylisocyanate was dropwise added thereto in a range of from -15° C. to -5°C. The reaction solution was heated to 0° C. and then further stirred atthe same temperature for 15 minutes. Then, the reaction solution wascooled again to -30° C., and a mixed solution comprising 1.56 g (12mmol) of 3,4,5,6-tetrahydro-3-methyl-2H-1,3-thiazin-2-imine, 1.21 g (12mmol) of triethylamine and 10 ml of dry tetrahydrofuran, was dropwiseadded thereto. The reaction solution was gradually heated to roomtemperature with stirring, and then the solvent was distilled off underreduced pressure. 80 ml of water was added to the residue, andprecipitated crystals were extracted three times with 60 ml ofchloroform. The chloroform layer was washed with water and dried overanhydrous sodium sulfate. Then, chloroform was distilled off underreduced pressure.

Obtained crystals were washed with a solvent mixture of ethylether/acetonitrile to obtain 1.2 g of desired1-(3,4,5,6-tetrahydro-3-methyl-2H-1,3-thiazine-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)urea.

Melting point: 188°-190° C.

The structures and the physical property values of the compoundsprepared by the same methods as in Examples e-1 and e-2 are presented inTables 14e-1 and 14e-2.

                                      TABLE 14e-1                                 __________________________________________________________________________     ##STR779##                                                                   Compound                        m.p.                                          No.   R.sup.e1                                                                            R.sup.e2                                                                         R.sup.e3                                                                         R.sup.e4                                                                         A  B   D   (°C.)                                  __________________________________________________________________________    3-e   CH.sub.3                                                                            H  H  H  CH OCH.sub.3                                                                         OCH.sub.3                                                                         194-196                                       4-e   CH.sub.2 OCH.sub.3                                                                  H  H  H  CH OCH.sub.3                                                                         OCH.sub.3                                                                         158-160                                       __________________________________________________________________________

                  TABLE 14e-2                                                     ______________________________________                                         ##STR780##                                                                   Com-                                                                          pound                                           m.p.                          No.   R.sup.e1                                                                              R.sup.e8                                                                             R.sup.e9                                                                           R.sup.e10                                                                          A    B     D     (°C.)                  ______________________________________                                        5-e   C.sub.3 H.sub.7 -n                                                                    H      H    H    CH   OCH.sub.3                                                                           OCH.sub.3                                                                           166-                                                                          167                           ______________________________________                                    

EXAMPLE f-1

Preparation of1-(3-methyloxazolidine-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)ure##STR781##

1.55 g (10 mmol) of 2-amino-4,6-dimethoxypyrimidine was dissolved in 30ml of dry tetrahydrofuran, and 1.42 g (10 mmol) of chlorosulfonylisocyanate was dropwise added thereto at -20° C. The reactiontemperature was raised to -5° C., and the mixture was stirred at thesame temperature for 5 minutes. The reaction mixture was cooled again to-20° C., and a mixture comprising 2.28 g (10 mmol) of2-imino-3-methyloxazolidine hydroiodide, 2.22 g (22 mmol) oftriethylamine and 30 ml of dry tetrahydrofuran, was added thereto. Thereaction temperature was raised to room temperature, and the mixture wasfurther stirred at the same temperature for one hour. Then, the solventwas distilled off under reduced pressure, and then 100 ml of water wasadded to the obtained residue. Precipitated crystals were collected byfiltration, washed with water and then with a solvent mixture of ethylether/acetonitrile and dried to obtain 0.8 g of desired1-(3-methyloxazolidine-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)urea.

Melting point: 174°-175° C.

The structures and the physical property values of the compoundsprepared by the same method as in Example f-1 are presented in Tables14f.

                                      TABLE 14f                                   __________________________________________________________________________     ##STR782##                                                                   Compound                        m.p.                                          No.   R.sup.f1 R.sup.f5                                                                         R.sup.f6                                                                         A  B   D   (°C.)                                  __________________________________________________________________________    2-f   CH.sub.2 CHCH.sub.2                                                                    H  H  CH OCH.sub.3                                                                         OCH.sub.3                                                                         157-159                                       __________________________________________________________________________

EXAMPLE g-1

Preparation of1-[N-((methylthio-N,N-dimethylamino)methylene)aminosulfonyl]-3-(4,6-dimethoxypyrimidin-2-yl)urea##STR783##

1.55 g (10 mmol) of 2-amino-4,6-dimethoxypyrimidine was dissolved in 40ml of dry tetrahydrofuran, and 1.42 g (10 mmol) of chlorosulfonylisocyanate was dropwise added thereto in a range of from -20° C. to -15°C. The reaction temperature was raised to 0° C., and the mixture wascooled again to -20° C. Then, a mixture comprising 2.5 g (10.2 mmol) ofN,N-dimethyl-S-methylisothiourea hydroiodide, 2.22 g (22 mmol) oftriethylamine and 30 ml of dry tetrahydrofuran, was added thereto. Thereaction temperature was raised to room temperature, and the mixture wasfurther stirred at the same temperature for 10 minutes. Then, thesolvent was distilled off under reduced pressure, and then 80 ml ofwater was added to the obtained residue. The mixture was extracted threetimes with 30 ml of chloroform. The chloroform layer was washed withwater and then dried over anhydrous sodium sulfate. Then, solvent wasdistilled off under reduced pressure. Obtained crystals were washed witha solvent mixture of ethyl ether/acetonitrile to obtain 2 g of desired1-[N-((methylthio-N,N-dimethylamino)methylene)aminosulfonyl]-3-(4,6-dimethoxypyrimidin-2-yl)urea.

Melting point: 167°-168° C.

EXAMPLE g-2

Preparation of1-[N-((methylthio-N-ethyl-N-methylamino)methylene)aminosulfonyl]-3-(4,6-dimethoxypyrimidin-2-yl)urea##STR784##

1.55 g (10 mmol) of 2-amino-4,6-dimethoxypyrimidine was dissolved in 40ml of dry tetrahydrofuran, and 1.42 g (10 mmol) of chlorosulfonylisocyanate was dropwise added thereto in a range of from -20° C. to -15°C. The reaction temperature was raised to 0° C., and the mixture wascooled again to -20° C. Then, a mixture comprising 2.60 g (10 mmol) ofN-ethyl-N-methyl-S-methylisothiourea hydroiodide, 2.22 g (22 mmol) oftriethylamine and 30 ml of dry tetrahydrofuran, was added thereto. Thereaction temperature was raised to room temperature, and the mixture wasfurther stirred at the same temperature for one hour. Then, the solventwas distilled off under reduced pressure, and 80 ml of water was addedto the obtained residue. The mixture was extracted three times with 50ml of chloroform. The chloroform layer was washed with water, and thendried over anhydrous sodium sulfate. Then, the solvent was distilled offunder reduced pressure. Obtained crystals were washed with acetonitrileto obtain 1.32 g of desired1-[N-((methylthio-N-ethyl-N-methylamino)methylene)aminosulfonyl]-3-(4,6-dimethoxypyrimidin-2-yl)urea.

Melting point: 143°-144° C.

EXAMPLE g-3

Preparation of1-[N-((methylthio-N-methoxy-N-methylamino)methylene)aminosulfonyl]-3-(4,6-dimethoxypyrimidin-2-yl)urea##STR785##

0.78 g (5 mmol) of 2-amino-4,6-dimethoxypyrimidine was dissolved in 20ml of dry tetrahydrofuran, and 0.71 g (5 mmol) of chlorosulfonylisocyanate was dropwise added thereto in a range of from -20° C. to -15°C. The reaction temperature was raised to 0° C., and then the mixturewas cooled again to -20° C. Then, a mixture comprising 1.31 g (5 mmol)of N-methoxy-N-methyl-S-methylisothiourea hydroiodide, 1.11 g (11 mmol)of triethylamine and 15 ml of dry tetrahydrofuran, was added thereto.The reaction temperature was raised to room temperature, and the mixturewas further stirred at the same temperature for one hour. Then, thesolvent was distilled off under reduced pressure, and then 40 ml ofwater was added to the obtained residue. The mixture was extracted threetimes with 25 ml of chloroform. The chloroform layer was washed withwater, and then dried over anhydrous sodium sulfate. Then, the solventwas distilled off under reduced pressure. Obtained crystals were washedwith acetonitrile to obtain 1.51 g of desired1-[N-((methylthio-N-methoxy-N-methylamino)methylene)aminosulfonyl]-3-(4,6-dimethoxypyrimidin-2-yl)urea.

Melting point: 165°-167° C.

The structures and the physical property values of the compoundsprepared by the same methods as in Examples g-1 to g-3 are presented inTable 14g.

                                      TABLE 14g                                   __________________________________________________________________________     ##STR786##                                                                   Compound                            m.p.                                      No.   R.sup.g1                                                                              R.sup.g2                                                                         R.sup.g3                                                                              A  B   D   (°C.)                              __________________________________________________________________________     2-g  C.sub.2 H.sub.5                                                                       CH.sub.3                                                                         CH.sub.3                                                                              CH OCH.sub.3                                                                         OCH.sub.3                                                                         129-130                                    3-g  C.sub.3 H.sub.7 -n                                                                    CH.sub.3                                                                         CH.sub.3                                                                              CH OCH.sub.3                                                                         OCH.sub.3                                                                         115-116                                    4-g  CH.sub.2 CHCH.sub.2                                                                   CH.sub.3                                                                         CH.sub.3                                                                              CH OCH.sub.3                                                                         OCH.sub.3                                                                         131-132                                    5-g  CH.sub.2 CCH                                                                          CH.sub.3                                                                         CH.sub.3                                                                              CH OCH.sub.3                                                                         OCH.sub.3                                                                         140-141                                    6-g  CH.sub.3                                                                              CH.sub.3                                                                         COCH.sub.3                                                                            CH OCH.sub.3                                                                         OCH.sub.3                                                                         162-164                                    8-g  CH.sub.3                                                                               (CH.sub.2).sub.4                                                                        CH OCH.sub.3                                                                         OCH.sub.3                                                                         184-186                                    9-g  CH.sub.3                                                                              CH.sub.3                                                                         C.sub.3 H.sub.7 -n                                                                    CH OCH.sub.3                                                                         OCH.sub.3                                                                         123-125                                   10-g  CH.sub.3                                                                              CH.sub.3                                                                         Ph      CH OCH.sub.3                                                                         OCH.sub.3                                                                         163-164                                   11-g  CH.sub.3                                                                              CH.sub.3                                                                         CH.sub.3                                                                              CH OCH.sub.3                                                                         CH.sub.3                                                                          178-179                                   13-g  CH.sub.3                                                                              CH.sub.3                                                                         OC.sub.2 H.sub.5                                                                      CH OCH.sub.3                                                                         OCH.sub.3                                                                         142-143                                   14-g  CH.sub.3                                                                              CH.sub.3                                                                         OC.sub.3 H.sub.7 -n                                                                   CH OCH.sub.3                                                                         OCH.sub.3                                                                         124-125                                   15-g  CH.sub.3                                                                              CH.sub.3                                                                         OC.sub.3 H.sub.7 -n                                                                   CH OCH.sub.3                                                                         CH.sub.3                                                                          142-143                                   16-g  CH.sub.3                                                                              CH.sub.3                                                                         OC.sub.2 H.sub.5                                                                      CH OCH.sub.3                                                                         CH.sub.3                                                                          141-142                                   17-g  CH.sub.3                                                                              CH.sub.3                                                                         OC.sub.2 H.sub.5                                                                      N  OCH.sub.3                                                                         CH.sub.3                                                                          148-149                                   18-g  CH.sub.3                                                                              CH.sub.3                                                                         OC.sub.3 H.sub.7 -n                                                                   N  OCH.sub.3                                                                         CH.sub.3                                                                          138-139                                   19-g  CH.sub.3                                                                              CH.sub.3                                                                         CH.sub.2 CHCH.sub.2                                                                   CH OCH.sub.3                                                                         OCH.sub.3                                                                         138-141                                   20-g  CH.sub.3                                                                              CH.sub.3                                                                         CH.sub.3                                                                              N  OCH.sub.3                                                                         CH.sub.3                                                                          166- 167                                  __________________________________________________________________________

Now, Formulation Examples of the herbicides containing the compounds ofthe present invention will be given specifically. However, it should beunderstood that the present invention is by no means restricted to suchspecific Examples. In the following Formulation Examples, "parts" means"parts by weight".

    ______________________________________                                        Wettable powder                                                               ______________________________________                                        Compound of the present invention                                                                   5-80 parts                                              Solid carrier         10-85 parts                                             Surfactant            1-10 parts                                              Other                 1-5 parts                                               ______________________________________                                    

As other, a coagulation preventing agent may, for example, be mentioned.

    ______________________________________                                        Emulsifiable concentrate                                                      ______________________________________                                        Compound of the present invention                                                                   1-30 parts                                              Liquid carrier        30-95 parts                                             Surfactant            5-15 parts                                              ______________________________________                                        Flowable                                                                      ______________________________________                                        Compound of the present invention                                                                   5-70 parts                                              Liquid carrier        15-65 parts                                             Surfactant            5-12 parts                                              Other                 5-30 parts                                              ______________________________________                                    

As other, an antifreezing agent and a thickener may, for example, bementioned.

    ______________________________________                                        Granular wettable powder (dry flowable)                                       ______________________________________                                        Compound of the present invention                                                                  20-90      parts                                         Solid carrier        10-60      parts                                         Surfactant           1-20       parts                                         ______________________________________                                        Granule                                                                       ______________________________________                                        Compound of the present invention                                                                  0.1-10     parts                                         Solid carrier        90-99.9    parts                                         Other                1-5        parts                                         ______________________________________                                    

FORMULATION EXAMPLE a-1: Wettable powder

    ______________________________________                                        Compound No. 1-a of the present invention                                                               20 parts                                            Zeeklite A (tradename for a kaolin-type                                                                 76 parts                                            clay, manufactured by Zeeklite Industries,                                    Co., Ltd.)                                                                    Sorpol 5039 (tradename for a mixture of a                                                                2 parts                                            nonionic surfactant and an anionic                                            surfactant, manufactured by Toho Chemical                                     Industry Co., Ltd.)                                                           Carplex (tradename for a coagulation-                                                                    2 parts                                            preventing agent composed of a white carbon,                                  manufactured by Shionogi Pharmaceutical                                       Co., Ltd.)                                                                    ______________________________________                                    

The above ingredients are homogeneously pulverized and mixed to form awettable powder.

FORMULATION EXAMPLE a-2: Wettable powder

    ______________________________________                                        Compound No. 2-a of the present invention                                                               40 parts                                            Zeeklite A (tradename for a kaolin-type                                                                 54 parts                                            clay, manufactured by Zeeklite Industries,                                    Co., Ltd.)                                                                    Sorpol 5039 (tradename for a mixture of a                                                                2 parts                                            nonionic surfactant and an anionic                                            surfactant, manufactured by Toho Chemical                                     Industry Co., Ltd.)                                                           Carplex (tradename for a coagulation-                                                                    4 parts                                            preventing agent composed of a white carbon,                                  manufactured by Shionogi Pharmaceutical                                       Co., Ltd.)                                                                    ______________________________________                                    

The above ingredients are homogeneously pulverized and mixed to form awettable powder.

FORMULATION EXAMPLE a-3: Emulsifiable concentrate

    ______________________________________                                        Compound No. 3-a of the present invention                                                               5 parts                                             Xylene                   75 parts                                             N,N-dimethylformamide    15 parts                                             Sorpol 2680 (tradename for a mixture of a                                                               5 parts                                             nonionic surfactant and an anionic                                            surfactant, manufactured by Toho Chemical                                     Industry Co., Ltd.)                                                           ______________________________________                                    

The above ingredients are homogeneously mixed to form an emulsifiableconcentrate.

FORMULATION EXAMPLE a-4: Flowable

    ______________________________________                                        Compound No. 7-a of the present invention                                                              25      parts                                        Agrizole S-710 (tradename for a nonionic                                                               10      parts                                        surfactant, manufactured by Kao Corp.)                                        Runox 1000C (tradename for an anionic                                                                  0.5     part                                         surfactant, manufactured by Toho Chemical                                     Industry Co., Ltd.)                                                           1% Rodopol water (tradename for a thickener,                                                           20      parts                                        manufactured by Rhone-Poulenc)                                                Water                    44.5    parts                                        ______________________________________                                    

The above ingredients were homogeneously mixed to obtain a flowable.

FORMULATION EXAMPLE a-5: Flowable

    ______________________________________                                        Compound No. 8-a of the present invention                                                              40      parts                                        Agrizole S-710 (tradename for a nonionic                                                               10      parts                                        surfactant, manufactured by Kao Corp.)                                        Runox 1000C (tradename for an anionic                                                                  0.5     part                                         surfactant, manufactured by Toho Chemical                                     Industry Co., Ltd.)                                                           1% Rodopol water (tradename for a thickener,                                                           20      parts                                        manufactured by Rhone-Poulenc)                                                Water                    29.5    parts                                        ______________________________________                                    

The above ingredients were homogeneously mixed to obtain a flowable.

FORMULATION EXAMPLE a-6: Granular wettable powder (dry flowable)

    ______________________________________                                        Compound No. 10-a of the present invention                                                              75 parts                                            Isoban No. 1 (tradename for an anionic                                                                  10 parts                                            surfactant, manufactured by Kuraray Isoprene                                  Chemical Co., Ltd.)                                                           Vanirex N (tradename for an anionic                                                                      5 parts                                            surfactant, manufactured by Sanyo Kokusaku                                    Pulp Co., Ltd.)                                                               Carplex #80 (tradename for a white carbon,                                                              10 parts                                            manufactured by Shionogi Pharmaceutical                                       Co., Ltd.)                                                                    ______________________________________                                    

The above ingredients are uniformly mixed and pulverized to form a dryflowable.

FORMULATION EXAMPLE a-7: Granule

    ______________________________________                                        Compound No. 69-a of the present invention                                                             1      part                                          Bentonite                55     parts                                         Talc                     44     parts                                         ______________________________________                                    

The above ingredients were homogeneously mixed and pulverized, and afteran addition of a small amount of water, the mixture was stirred, mixedand granulated by an extrusion-type granulating machine, followed bydrying to obtain a granule.

FORMULATION EXAMPLE b-1: Wettable powder

    ______________________________________                                        Compound No. 1-b of the present invention                                                               20 parts                                            Zeeklite A (tradename for a kaolin-type                                                                 76 parts                                            clay, manufactured by Zeeklite Industries,                                    Co., Ltd.)                                                                    Sorpol 5039 (tradename for a mixture of a                                                                2 parts                                            nonionic surfactant and an anionic                                            surfactant, manufactured by Toho Chemical                                     Industry Co., Ltd.)                                                           Carplex (tradename for a coagulation-                                                                    2 parts                                            preventing agent composed of a white carbon,                                  manufactured by Shionogi Pharmaceutical                                       Co., Ltd.)                                                                    ______________________________________                                    

The above ingredients are homogeneously pulverized and mixed to form awettable powder.

FORMULATION EXAMPLE b-2: Wettable powder

    ______________________________________                                        Compound No. 2-b of the present invention                                                               40 parts                                            Zeeklite A (tradename for a kaolin-type                                                                 54 parts                                            clay, manufactured by Zeeklite Industries,                                    Co., Ltd.)                                                                    Sorpol 5039 (tradename for a mixture of a                                                                2 parts                                            nonionic surfactant and an anionic                                            surfactant, manufactured by Toho Chemical                                     Industry Co., Ltd.)                                                           Carplex (tradename for a coagulation-                                                                    4 parts                                            preventing agent composed of a white carbon,                                  manufactured by Shionogi Pharmaceutical                                       Co., Ltd.)                                                                    ______________________________________                                    

The above ingredients are homogeneously pulverized and mixed to form awettable powder.

FORMULATION EXAMPLE b-3: Emulsifiable concentrate

    ______________________________________                                        Compound No. 3-b of the present invention                                                               5 parts                                             Xylene                   75 parts                                             N,N-dimethylformamide    15 parts                                             Sorpol 2680 (tradename for a mixture of a                                                               5 parts                                             nonionic surfactant and an anionic                                            surfactant, manufactured by Toho Chemical                                     Industry Co., Ltd.)                                                           ______________________________________                                    

The above ingredients are homogeneously mixed to form an emulsifiableconcentrate.

FORMULATION EXAMPLE b-4: Flowable

    ______________________________________                                        Compound No. 1-b of the present invention                                                              25      parts                                        Agrizole S-710 (tradename for a nonionic                                                               10      parts                                        surfactant, manufactured by Kao Corp.)                                        Runox 1000C (tradename for an anionic                                                                  0.5     part                                         surfactant, manufactured by Toho Chemical                                     Industry Co., Ltd.)                                                           1% Rodopol water (tradename for a thickener,                                                           20      parts                                        manufactured by Rhone-Poulenc)                                                Water                    44.5    parts                                        ______________________________________                                    

The above ingredients were homogeneously mixed to obtain a flowable.

FORMULATION EXAMPLE b-5: Flowable

    ______________________________________                                        Compound No. 4-b of the present invention                                                              40      parts                                        Agrizole S-710 (tradename for a nonionic                                                               10      parts                                        surfactant, manufactured by Kao Corp.)                                        Runox 1000C (tradename for an anionic                                                                  0.5     part                                         surfactant, manufactured by Toho Chemical                                     Industry Co., Ltd.)                                                           1% Rodopol water (tradename for a thickener,                                                           20      parts                                        manufactured by Rhone-Poulenc)                                                Water                    29.5    parts                                        ______________________________________                                    

The above ingredients were homogeneously mixed to obtain a flowable.

FORMULATION EXAMPLE b-6: Granular wettable powder (dry flowable)

    ______________________________________                                        Compound No. 5-b of the present invention                                                               75 parts                                            Isoban No. 1 (tradename for an anionic                                                                  10 parts                                            surfactant, manufactured by Kuraray Isoprene                                  Chemical Co., Ltd.)                                                           Vanirex N (tradename for an anionic                                                                      5 parts                                            surfactant, manufactured by Sanyo Kokusaku                                    Pulp Co., Ltd.)                                                               Carplex #80 (tradename for a white carbon,                                                              10 parts                                            manufactured by Shionogi Pharmaceutical                                       Co., Ltd.)                                                                    ______________________________________                                    

The above ingredients are uniformly mixed and pulverized to form a dryflowable.

FORMULATION EXAMPLE b-7: Granule

    ______________________________________                                        Compound No. 6-b of the present invention                                                               1     part                                          Bentonite                 55    parts                                         Talc                      44    parts                                         ______________________________________                                    

The above ingredients were homogeneously mixed and pulverized, and afteran addition of a small amount of water, the mixture was stirred, mixedand granulated by an extrusion-type granulating machine, followed bydrying to obtain a granule.

FORMULATION EXAMPLE c-1: Wettable powder

    ______________________________________                                        Compound No. 1-c of the present invention                                                               20 parts                                            Zeeklite A (tradename for a kaolin-type                                                                 76 parts                                            clay, manufactured by Zeeklite Industries,                                    Co., Ltd.)                                                                    Sorpol 5039 (tradename for a mixture of a                                                                2 parts                                            nonionic surfactant and an anionic                                            surfactant, manufactured by Toho Chemical                                     Industry Co., Ltd.)                                                           Carplex (tradename for a coagulation-                                                                    2 parts                                            preventing agent composed of a white carbon,                                  manufactured by Shionogi Pharmaceutical                                       Co., Ltd.)                                                                    ______________________________________                                    

The above ingredients are homogeneously pulverized and mixed to form awettable powder.

FORMULATION EXAMPLE c-2: Wettable powder

    ______________________________________                                        Compound No. 2-c of the present invention                                                               40 parts                                            Zeeklite A (tradename for a kaolin-type                                                                 54 parts                                            clay, manufactured by Zeeklite Industries,                                    Co., Ltd.)                                                                    Sorpol 5039 (tradename for a mixture of a                                                                2 parts                                            nonionic surfactant and an anionic                                            surfactant, manufactured by Toho Chemical                                     Industry Co., Ltd.)                                                           Carplex (tradename for a coagulation-                                                                    4 parts                                            preventing agent composed of a white carbon,                                  manufactured by Shionogi Pharmaceutical                                       Co., Ltd.)                                                                    ______________________________________                                    

The above ingredients are homogeneously pulverized and mixed to form awettable powder.

FORMULATION EXAMPLE c-3: Emulsifiable concentrate

    ______________________________________                                        Compound No. 12-c of the present invention                                                              5 parts                                             Xylene                   75 parts                                             N,N-dimethylformamide    15 parts                                             Sorpol 2680 (tradename for a mixture of a                                                               5 parts                                             nonionic surfactant and an anionic                                            surfactant, manufactured by Toho Chemical                                     Industry Co., Ltd.)                                                           ______________________________________                                    

The above ingredients are homogeneously mixed to form an emulsifiableconcentrate.

FORMULATION EXAMPLE c-4: Flowable

    ______________________________________                                        Compound No. 24-c of the present invention                                                             25      parts                                        Agrizole S-710 (tradename for a nonionic                                                               10      parts                                        surfactant, manufactured by Kao Corp.)                                        Runox 1000C (tradename for an anionic                                                                  0.5     part                                         surfactant, manufactured by Toho Chemical                                     Industry Co., Ltd.)                                                           1% Rodopol water (tradename for a thickener,                                                           20      parts                                        manufactured by Rhone-Poulenc)                                                Water                    44.5    parts                                        ______________________________________                                    

The above ingredients were homogeneously mixed to obtain a flowable.

FORMULATION EXAMPLE c-5: Flowable

    ______________________________________                                        Compound No. 37-c of the present invention                                                             40      parts                                        Agrizole S-710 (tradename for a nonionic                                                               10      parts                                        surfactant, manufactured by Kao Corp.)                                        Runox 1000C (tradename for an anionic                                                                  0.5     part                                         surfactant, manufactured by Toho Chemical                                     Industry Co., Ltd.)                                                           1% Rodopol water (tradename for a thickener,                                                           20      parts                                        manufactured by Rhone-Poulenc)                                                Water                    29.5    parts                                        ______________________________________                                    

The above ingredients were homogeneously mixed to obtain a flowable.

FORMULATION EXAMPLE c-6: Granular wettable powder (dry flowable)

    ______________________________________                                        Compound No. 45-c of the present invention                                                             75      parts                                        Isoban No. 1 (tradename for an anionic                                                                 10      parts                                        surfactant, manufactured by Kuraray Isoprene                                  Chemical Co., Ltd.)                                                           Vanirex N (tradename for an anionic                                                                    5       parts                                        surfactant, manufactured by Sanyo Kokusaku                                    Pulp Co., Ltd.)                                                               Carplex #80 (tradename for a white carbon,                                                             10      parts                                        manufactured by Shionogi Pharmaceutical                                       Co., Ltd.)                                                                    ______________________________________                                    

The above ingredients are uniformly mixed and pulverized to form a dryflowable.

FORMULATION EXAMPLE c-7: Granule

    ______________________________________                                        Compound No. 48-c of the present invention                                                             1      part                                          Bentonite                55     parts                                         Talc                     44     parts                                         ______________________________________                                    

The above ingredients were homogeneously mixed and pulverized, and afteran addition of a small amount of water, the mixture was stirred, mixedand granulated by an extrusion-type granulating machine, followed bydrying to obtain a granule.

FORMULATION EXAMPLE d-1: Wettable powder

    ______________________________________                                        Compound No. 1-d of the present invention                                                               20 parts                                            Zeeklite A (tradename for a kaolin-type                                                                 76 parts                                            clay, manufactured by Zeeklite Industries,                                    Co., Ltd.)                                                                    Sorpol 5039 (tradename for a mixture of a                                                                2 parts                                            nonionic surfactant and an anionic                                            surfactant, manufactured by Toho Chemical                                     Industry Co., Ltd.)                                                           Carplex (tradename for a coagulation-                                                                    2 parts                                            preventing agent composed of a white carbon                                   manufactured by Shionogi Pharmaceutical                                       Co., Ltd.)                                                                    ______________________________________                                    

The above ingredients are homogeneously pulverized and mixed to form awettable powder.

FORMULATION EXAMPLE d-2: Wettable powder

    ______________________________________                                        Compound No. 2-d of the present invention                                                               40 parts                                            Zeeklite A (tradename for a kaolin-type                                                                 54 parts                                            clay, manufactured by Zeeklite Industries,                                    Co., Ltd.)                                                                    Sorpol 5039 (tradename for a mixture of a                                                                2 parts                                            nonionic surfactant and an anionic                                            surfactant, manufactured by Toho Chemical                                     Industry Co., Ltd.)                                                           Carplex (tradename for a coagulation-                                                                    4 parts                                            preventing agent composed of a white carbon,                                  manufactured by Shionogi Pharmaceutical                                       Co., Ltd.)                                                                    ______________________________________                                    

The above ingredients are homogeneously pulverized and mixed to form awettable powder.

FORMULATION EXAMPLE d-3: Emulsifiable concentrate

    ______________________________________                                        Compound No. 3-d of the present invention                                                               5 parts                                             Xylene                   75 parts                                             N,N-dimethylformamide    15 parts                                             Sorpol 2680 (tradename for a mixture of a                                                               5 parts                                             nonionic surfactant and an anionic                                            surfactant, manufactured by Toho Chemical                                     Industry Co., Ltd.)                                                           ______________________________________                                    

The above ingredients are homogeneously mixed to form an emulsifiableconcentrate.

FORMULATION EXAMPLE d-4: Flowable

    ______________________________________                                        Compound No. 4-d of the present invention                                                              25      parts                                        Agrizole S-710 (tradename for a nonionic                                                               10      parts                                        surfactant, manufactured by Kao Corp.)                                        Runox 1000C (tradename for an anionic                                                                  0.5     part                                         surfactant, manufactured by Toho Chemical                                     Industry Co., Ltd.)                                                           1% Rodopol water (tradename for a thickener,                                                           20      parts                                        manufactured by Rhone-Poulenc)                                                Water                    44.5    parts                                        ______________________________________                                    

The above ingredients were homogeneously mixed to obtain a flowable.

FORMULATION EXAMPLE d-5: Flowable

    ______________________________________                                        Compound No. 5-d of the present invention                                                              40      parts                                        Agrizole S-710 (tradename for a nonionic                                                               10      parts                                        surfactant, manufactured by Kao Corp.)                                        Runox 1000C (tradename for an anionic                                                                  0.5     part                                         surfactant, manufactured by Toho Chemical                                     Industry Co., Ltd.)                                                           1% Rodopol water (tradename for a thickener,                                                           20      parts                                        manufactured by Rhone-Poulenc)                                                Water                    29.5    parts                                        ______________________________________                                    

The above ingredients were homogeneously mixed to obtain a flowable.

FORMULATION EXAMPLE d-6: Granular wettable powder (dry flowable)

    ______________________________________                                        Compound No. 6-d of the present invention                                                               75 parts                                            Isoban No. 1 (tradename for an anionic                                                                  10 parts                                            surfactant, manufactured by Kuraray Isoprene                                  Chemical Co., Ltd.)                                                           Vanirex N (tradename for an anionic                                                                      5 parts                                            surfactant, manufactured by Sanyo Kokusaku                                    Pulp Co., Ltd.)                                                               Carplex #80 (tradename for a white carbon,                                                              10 parts                                            manufactured by Shionogi Pharmaceutical                                       Co., Ltd.)                                                                    ______________________________________                                    

The above ingredients are uniformly mixed and pulverized to form a dryflowable.

FORMULATION EXAMPLE d-7: Granule

    ______________________________________                                        Compound No. 9-d of the present invention                                                               1     part                                          Bentonite                 55    parts                                         Talc                      44    parts                                         ______________________________________                                    

The above ingredients were homogeneously mixed and pulverized, and afteran addition of a small amount of water, the mixture was stirred, mixedand granulated by an extrusion-type granulating machine, followed bydrying to obtain a granule.

FORMULATION EXAMPLE e-1: Wettable powder

    ______________________________________                                        Compound No. 1-e of the present invention                                                               20 parts                                            Zeeklite A (tradename for a kaolin-type                                                                 76 parts                                            clay, manufactured by Zeeklite Industries,                                    Co., Ltd.)                                                                    Sorpol 5039 (tradename for a mixture of a                                                                2 parts                                            nonionic surfactant and an anionic                                            surfactant, manufactured by Toho Chemical                                     Industry Co., Ltd.)                                                           Carplex (tradename for a coagulation-                                                                    2 parts                                            preventing agent composed of a white carbon,                                  manufactured by Shionogi Pharmaceutical                                       Co., Ltd.)                                                                    ______________________________________                                    

The above ingredients are homogeneously pulverized and mixed to form awettable powder.

FORMULATION EXAMPLE e-2: Wettable powder

    ______________________________________                                        Compound No. 2-e of the present invention                                                               40 parts                                            Zeeklite A (tradename for a kaolin-type                                                                 54 parts                                            clay, manufactured by Zeeklite Industries,                                    Co., Ltd.)                                                                    Sorpol 5039 (tradename for a mixture of a                                                                2 parts                                            nonionic surfactant and an anionic                                            surfactant, manufactured by Toho Chemical                                     Industry Co., Ltd.)                                                           Carplex (tradename for a coagulation-                                                                    4 parts                                            preventing agent composed of a white carbon,                                  manufactured by Shionogi Pharmaceutical                                       Co., Ltd.)                                                                    ______________________________________                                    

The above ingredients are homogeneously pulverized and mixed to form awettable powder.

FORMULATION EXAMPLE e-3: Emulsifiable concentrate

    ______________________________________                                        Compound No. 3-e of the present invention                                                                5 parts                                            Xylene                    75 parts                                            N,N-dimethylformamide     15 parts                                            Sorpol 2680 (tradename for a mixture of a                                                                5 parts                                            nonionic surfactant and an anionic                                            surfactant, manufactured by Toho Chemical                                     Industry Co., Ltd.)                                                           ______________________________________                                    

The above ingredients are homogeneously mixed to form an emulsifiableconcentrate.

FORMULATION EXAMPLE e-4: Flowable

    ______________________________________                                        Compound No. 4-e of the present invention                                                               25     parts                                        Agrizole S-710 (tradename for a nonionic                                                                10     parts                                        surfactant, manufactured by Kao Corp.)                                        Runox 1000C (tradename for an anionic                                                                   0.5    part                                         surfactant, manufactured by Toho Chemical                                     Industry Co., Ltd.)                                                           1% Rodopol water (tradename for a thickener,                                                            20     parts                                        manufactured by Rhone-Poulenc)                                                Water                     44.5   parts                                        ______________________________________                                    

The above ingredients were homogeneously mixed to obtain a flowable.

FORMULATION EXAMPLE e-5: Flowable

    ______________________________________                                        Compound No. 5-e of the present invention                                                               40     parts                                        Agrizole S-710 (tradename for a nonionic                                                                10     parts                                        surfactant, manufactured by Kao Corp.)                                        Runox 1000C (tradename for an anionic                                                                   0.5    part                                         surfactant, manufactured by Toho Chemical                                     Industry Co., Ltd.)                                                           1% Rodopol water (tradename for a thickener,                                                            20     parts                                        manufactured by Rhone-Poulenc)                                                Water                     29.5   parts                                        ______________________________________                                    

The above ingredients were homogeneously mixed to obtain a flowable.

FORMULATION EXAMPLE e-6: Granular wettable powder (dry flowable)

    ______________________________________                                        Compound No. 1-e of the present invention                                                               75 parts                                            Isoban No. 1 (tradename for an anionic                                                                  10 parts                                            surfactant, manufactured by Kuraray Isoprene                                  Chemical Co., Ltd.)                                                           Vanirex N (tradename for an anionic                                                                      5 parts                                            surfactant, manufactured by Sanyo Kokusaku                                    Pulp Co., Ltd.)                                                               Carplex #80 (tradename for a white carbon,                                                              10 parts                                            manufactured by Shionogi Pharmaceutical                                       Co., Ltd.)                                                                    ______________________________________                                    

The above ingredients are uniformly mixed and pulverized to form a dryflowable.

FORMULATION EXAMPLE e-7: Granule

    ______________________________________                                        Compound No. 5-e of the present invention                                                              1       part                                         Bentonite                55      parts                                        Talc                     44      parts                                        ______________________________________                                    

The above ingredients were homogeneously mixed and pulverized, and afteran addition of a small amount of water, the mixture was stirred, mixedand granulated by an extrusion-type granulating machine, followed bydrying to obtain a granule.

FORMULATION EXAMPLE f-1: Wettable powder

    ______________________________________                                        Compound No. 1-f of the present invention                                                               20 parts                                            Zeeklite A (tradename for a kaolin-type                                                                 76 parts                                            clay, manufactured by Zeeklite Industries,                                    Co., Ltd.)                                                                    Sorpol 5039 (tradename for a mixture of a                                                                2 parts                                            nonionic surfactant and an anionic                                            surfactant, manufactured by Toho Chemical                                     Industry Co., Ltd.)                                                           Carplex (tradename for a coagulation-                                                                    2 parts                                            preventing agent composed of a white carbon,                                  manufactured by Shionogi Pharmaceutical                                       Co., Ltd.)                                                                    ______________________________________                                    

The above ingredients are homogeneously pulverized and mixed to form awettable powder.

FORMULATION EXAMPLE f-2: Wettable powder

    ______________________________________                                        Compound No. 2-f of the present invention                                                               40 parts                                            Zeeklite A (tradename for a kaolin-type                                                                 54 parts                                            clay, manufactured by Zeeklite Industries,                                    Co., Ltd.)                                                                    Sorpol 5039 (tradename for a mixture of a                                                                2 parts                                            nonionic surfactant and an anionic                                            surfactant, manufactured by Toho Chemical                                     Industry Co., Ltd.)                                                           Carplex (tradename for a coagulation-                                                                    4 parts                                            preventing agent composed of a white carbon,                                  manufactured by Shionogi Pharmaceutical                                       Co., Ltd.)                                                                    ______________________________________                                    

The above ingredients are homogeneously pulverized and mixed to form awettable powder.

FORMULATION EXAMPLE f-3: Emulsifiable concentrate

    ______________________________________                                        Compound No. 1-f of the present invention                                                               5 parts                                             Xylene                   75 parts                                             N,N-dimethylformamide    15 parts                                             Sorpol 2680 (tradename for a mixture of a                                                               5 parts                                             nonionic surfactant and an anionic                                            surfactant, manufactured by Toho Chemical                                     Industry Co., Ltd.)                                                           ______________________________________                                    

The above ingredients are homogeneously mixed to form an emulsifiableconcentrate.

FORMULATION EXAMPLE f-4: Flowable

    ______________________________________                                        Compound No. 2-f of the present invention                                                              25      parts                                        Agrizole S-710 (tradename for a nonionic                                                               10      parts                                        surfactant, manufactured by Kao Corp.)                                        Runox 1000C (tradename for an anionic                                                                  0.5     part                                         surfactant, manufactured by Toho Chemical                                     Industry Co., Ltd.)                                                           1% Rodopol water (tradename for a thickener,                                                           20      parts                                        manufactured by Rhone-Poulenc)                                                Water                    44.5    parts                                        ______________________________________                                    

The above ingredients were homogeneously mixed to obtain a flowable.

FORMULATION EXAMPLE f-5: Flowable

    ______________________________________                                        Compound No. 2-f of the present invention                                                              40      parts                                        Agrizole S-710 (tradename for a nonionic                                                               10      parts                                        surfactant, manufactured by Kao Corp.)                                        Runox 1000C (tradename for an anionic                                                                  0.5     part                                         surfactant, manufactured by Toho Chemical                                     Industry Co., Ltd.)                                                           1% Rodopol water (tradename for a thickener,                                                           20      parts                                        manufactured by Rhone-Poulenc)                                                Water                    29.5    parts                                        ______________________________________                                    

The above ingredients were homogeneously mixed to obtain a flowable.

FORMULATION EXAMPLE f-6: Granular wettable powder (dry flowable)

    ______________________________________                                        Compound No. 2-f of the present invention                                                               75 parts                                            Isoban No. 1 (tradename for an anionic                                                                  10 parts                                            surfactant, manufactured by Kuraray Isoprene                                  Chemical Co., Ltd.)                                                           Vanirex N (tradename for an anionic                                                                      5 parts                                            surfactant, manufactured by Sanyo Kokusaku                                    Pulp Co., Ltd.)                                                               Carplex #80 (tradename for a white carbon,                                                              10 parts                                            manufactured by Shionogi Pharmaceutical                                       Co., Ltd.)                                                                    ______________________________________                                    

The above ingredients are uniformly mixed and pulverized to form a dryflowable.

FORMULATION EXAMPLE f-7: Granule

    ______________________________________                                        Compound No. 2-f of the present invention                                                              1      part                                          Bentonite                55     parts                                         Talc                     44     parts                                         ______________________________________                                    

The above ingredients were homogeneously mixed and pulverized, and afteran addition of a small amount of water, the mixture was stirred, mixedand granulated by an extrusion-type granulating machine, followed bydrying to obtain a granule.

FORMULATION EXAMPLE g-1: Wettable powder

    ______________________________________                                        Compound No. 1-g of the present invention                                                                20    parts                                        Zeeklite A (tradename for a kaolin-type                                                                  76    parts                                        clay, manufactured by Zeeklite Industries,                                    Co., Ltd.)                                                                    Sorpol 5039 (tradename for a mixture of a                                                                2     parts                                        nonionic surfactant and an anionic                                            surfactant, manufactured by Toho Chemical                                     Industry Co., Ltd.)                                                           Carplex (tradename for a coagulation-                                                                    2     parts                                        preventing agent composed of a white carbon,                                  manufactured by Shionogi Pharmaceutical                                       Co., Ltd.)                                                                    ______________________________________                                    

The above ingredients are homogeneously pulverized and mixed to form awettable powder.

FORMULATION EXAMPLE g-2: Wettable powder

    ______________________________________                                        Compound No. 2-g of the present invention                                                                40    parts                                        Zeeklite A (tradename for a kaolin-type                                                                  54    parts                                        clay, manufactured by Zeeklite Industries,                                    Co., Ltd.)                                                                    Sorpol 5039 (tradename for a mixture of a                                                                2     parts                                        nonionic surfactant and an anionic                                            surfactant, manufactured by Toho Chemical                                     Industry Co., Ltd.)                                                           Carplex (tradename for a coagulation-                                                                    4     parts                                        preventing agent composed of a white carbon,                                  manufactured by Shionogi Pharmaceutical                                       Co., Ltd.)                                                                    ______________________________________                                    

The above ingredients are homogeneously pulverized and mixed to form awettable powder.

FORMULATION EXAMPLE g-3: Emulsifiable concentrate

    ______________________________________                                        Compound No. 3-g of the present invention                                                               5     parts                                         Xylene                    75    parts                                         N,N-dimethylformamide     15    parts                                         Sorpol 2680 (tradename for a mixture of a                                                               5     parts                                         nonionic surfactant and an anionic                                            surfactant, manufactured by Toho Chemical                                     Industry Co., Ltd.)                                                           ______________________________________                                    

The above ingredients are homogeneously mixed to form an emulsifiableconcentrate.

FORMULATION EXAMPLE g-4: Flowable

    ______________________________________                                        Compound No. 4-g of the present invention                                                              25      parts                                        Agrizole S-710 (tradename for a nonionic                                                               10      parts                                        surfactant, manufactured by Kao Corp.)                                        Runox 1000C (tradename for an anionic                                                                  0.5     part                                         surfactant, manufactured by Toho Chemical                                     Industry Co., Ltd.)                                                           1% Rodopol water (tradename for a thickener,                                                           20      parts                                        manufactured by Rhone-Poulenc)                                                Water                    44.5    parts                                        ______________________________________                                    

The above ingredients were homogeneously mixed to obtain a flowable.

FORMULATION EXAMPLE g-5: Flowable

    ______________________________________                                        Compound No. 5-g of the present invention                                                              40      parts                                        Agrizole S-710 (tradename for a nonionic                                                               10      parts                                        surfactant, manufactured by Kao Corp.)                                        Runox 1000C (tradename for an anionic                                                                  0.5     part                                         surfactant, manufactured by Toho Chemical                                     Industry Co., Ltd.)                                                           1% Rodopol water (tradename for a thickener,                                                           20      parts                                        manufactured by Rhone-Poulenc)                                                Water                    29.5    parts                                        ______________________________________                                    

The above ingredients were homogeneously mixed to obtain a flowable.

FORMULATION EXAMPLE g-6: Granular wettable powder (dry flowable)

    ______________________________________                                        Compound No. 12-g of the present invention                                                               75    parts                                        Isoban No. 1 (tradename for an anionic                                                                   10    parts                                        surfactant, manufactured by Kuraray Isoprene                                  Chemical Co., Ltd.)                                                           Vanirex N (tradename for an anionic                                                                      5     parts                                        surfactant, manufactured by Sanyo Kokusaku                                    Pulp Co., Ltd.)                                                               Carplex #80 (tradename for a white carbon,                                                               10    parts                                        manufactured by Shionogi Pharmaceutical                                       Co., Ltd.)                                                                    ______________________________________                                    

The above ingredients are uniformly mixed and pulverized to form a dryflowable.

FORMULATION EXAMPLE g-7: Granule

    ______________________________________                                        Compound No. 19-g of the present invention                                                              1     part                                          Bentonite                 55    parts                                         Talc                      44    parts                                         ______________________________________                                    

The above ingredients were homogeneously mixed and pulverized, and afteran addition of a small amount of water, the mixture was stirred, mixedand granulated by an extrusion-type granulating machine, followed bydrying to obtain a granule.

In use, the above wettable powder, emulsifiable concentrate, flowable orgranular wettable powder is diluted with water from 50 to 1,000 timesand applied so that the active ingredient will be from 0.0001 to 10 kgper hectare (ha).

Now, the herbicidal activities of the compounds of the present inventionwill be described in detail with reference to the following TestExamples.

TEST EXAMPLE 1: Test-1 on the herbicidal effects in soil treatment

A plastic box having a length of 15 cm, a width of 22 cm and a depth of6 cm was filled with a sterilized diluvial soil, and seeds ofEchinochloa crus-galli, Digitaria adscendens, Cyperus microiria, Solanumnigrum, Galinsoga ciliata, Rorippa indica, Oryza sativa, Zea mays,Triticum aestivum, Glycine max and Gossypium spp. were sown, and thesoil was covered thereon in a thickness of about 1.5 cm, and then aherbicide solution was applied onto the surface of the soil uniformly sothat the active ingredient was distributed at a predeterminedconcentration. The herbicide solution was prepared by diluting awettable powder prepared in accordance with the foregoing FormulationExamples with water and applied by a small spray onto the entire soilsurface. Four weeks after the application of the herbicidal solution,the herbicidal effects against each weed and the phytotoxicities againsteach crop plant were determined on the basis of the following standardratings. The results are shown in Table 15.

Standard ratings:

5: Growth control rate of more than 90% (almost completely withered)

4: Growth control rate of from 70 to 90%

3: Growth control rate of from 40 to 70%

2: Growth control rate of from 20 to 40%

1: Growth control rate of from 5 to 20%

0: Growth control rate of less than 5% (almost non-effective)

The above growth control rates were calculated by the followingequation: ##EQU1## where T: Weight of the weed grown above the soilsurface of the treated area

N: Weight of the weed grown above the soil surface of the non-treatedarea

TEST EXAMPLE 2: Test-1 on the herbicidal effects in foliage treatment

A plastic box having a length of 15 cm, a width of 22 cm and a depth of6 cm was filled with a sterilized diluvial soil, and seeds ofEchinochloa crus-galli, Digitaria adscendens, Avena fatua, Cyperusmicroiria, Solanum nigrum, Galinsoga ciliata, Rorippa indica, Oryzasativa, Zea mays, Triticum aestivum, Glycine max, Gossypium spp. andBeta vulgaris were spot-wisely sown, and the soil was covered thereon ina thickness of about 1.5 cm. When the various weeds and crop plants grewto the 2 or 3 leaf stage, a herbicidal solution was uniformly sprayed onthe foliages so that the active ingredient was applied in apredetermined concentration. The herbicidal solution was prepared bydiluting a wettable powder prepared in accordance with the aboveFormulation Examples with water and applied onto the entire surface ofthe foliages of the weeds and the crop plants by a small spray. Fourweeks after the application of the herbicide solution, the herbicidaleffects against each weed and the phytotoxicities against each cropplant were determined on the basis of the standard ratings described inTest Example 1. The results are shown in Table 16.

TEST EXAMPLE 3: Test-1 on the herbicidal effects in irrigation treatment

Into a Wagner pot of 1/5000a, alluvial soil was put, and then water wasintroduced and mixed to form an irrigated state with a water depth of 4cm. Seeds of Echinochloa crus-galli, Scirpus juncoides, Monochoriavaginalis and Rotala indica were sown in the above pot, and tubers ofSagittaria pygmaea and Cyperus serotinus were embedded. Then, riceseedlings of 2.5 leaf stage were transplanted. The pot was placed in agreenhouse at a temperature of from 25° to 30° C., and the plants werecultured. On the third day after the seeding and plantation, a dilutedsolution of the herbicide was dropwise applied to the water surface by ameasuring pipette, so that the dose would be a predetermined level.Three weeks after the dropwise application of the herbicide, theherbicidal effects against various weeds and rice were determined on thebasis of the standard ratings described in Test Example 1. The resultsare shown in Table 17.

In Tables 15, 16 and 17, Compound Nos. correspond to Compound Nos. inthe Examples, and symbols have the following meanings.

A: Echinochloa crus-galli (barnyardgrass)

B: Digitaria adscendens (large crabgrass)

C: Avena fatua (wild oat)

D: Cyperus microiria (annual sedge)

E: Solanum nigrum (black nightshade)

F: Galinsoga ciliata (hairy galinsoga)

G: Rorippa indica (fieldcress)

H: Scirpus juncoides (bulrush)

I: Monochoria vaginalis (ducksalad)

J: Rotala indica (toothcup)

K: Sagittaria pygmaea (arrowhead)

L: Cyperus serotinus (flat sedge)

a: Oryza sativa (rice)

b: Zea mays (corn)

c: Triticum aestivum (wheat)

d: Glycine max (soybean)

e: Gossypium spp. (cotton)

f: Beta vulgaris (sugar beet)

    ______________________________________                                              Dose                                                                                                 No. (kg/ha) A B D E F G a b c d e                ______________________________________                                         1-a  2.5      4     4   5   1   3   5   5   5   5   4                                                     3                                                                              2-a 0.04 5 5 5 1 5 5 1 0 0 0 0                                                0.08 5 5 5 1 5 5 2 1 1 0 0                                                    0.16 5 5 5 2 5 5 3 3 2 1 0                                                    3-a 2.5 4 4 1 1 0 4 3 0 2 1 0                                                 6-a 0.63 5 5 5 0 4 4 4 1 3 0 0                                                7-a 0.04 4 5 5 0 3 4 0 0 0 0 0                                                0.08 5 5 5 0 4 5 0 0 0 0 0                                                    0.16 5 5 5 2 5 5 2 0 0 0 0                                                    8-a 0.63 5 5 5 2 5 5 3 0 0 0 0                                               10-a 0.16 4 5 5 0 2 4 0 0 0 0 0                                                0.32 5 5 5 0 4 5 1 0 0 0 0                                                    0.63 5 5 5 0 5 5 3 0 0 0 0                                                   12-a 0.04 5 4 4 0 3 5 0 0 0 0 0                                                0.08 5 5 5 0 4 5 1 0 0 0 0                                                    0.16 5 5 5 1 5 5 3 1 0 0 0                                                   20-a 0.04 4 2 5 0 3 3 1 0 0 0 0                                                0.08 5 3 5 0 4 4 2 0 0 0 0                                                    0.16 5 4 5 1 5 5 3 1 0 0 0                                                   22-a 0.16 5 2 5 0 5 5 0 0 0 0 0                                                0.32 5 3 5 1 5 5 0 0 0 0 0                                                    0.63 5 4 5 1 5 5 1 0 0 0 0                                                   24-a 0.16 5 5 4 0 3 4 0 0 0 0 0                                                0.32 5 5 5 0 4 5 2 0 0 0 0                                                    0.63 5 5 5 0 5 5 3 1 1 0 0                                                   25-a 0.63 5 5 5 2 4 5 3 1 1 0 0                                               26-a 0.63 4 3 4 0 4 5 0 0 0 0 0                                               30-a 2.5 3 2 5 4 5 5 4 3 2 1 0                                                31-a 2.5 2 2 5 4 4 5 2 0 1 0 0                                                34-a 2.5 5 5 5 4 5 5 3 3 5 0 0                                                36-a 2.5 5 4 5 5 5 5 1 0 0 0 0                                                38-a 0.63 5 5 5 2 4 5 2 1 0 0 0                                               39-a 2.5 5 5 5 4 4 5 3 1 0 0 0                                                40-a 0.63 5 5 5 3 4 5 2 1 1 0 0                                               41-a 2.5 5 5 5 4 5 5 4 4 1 1 0                                                43-a 2.5 3 4 5 3 3 5 0 0 0 0 0                                                45-a 0.63 5 5 5 0 5 5 0 0 0 0 0                                               47-a 0.63 5 4 5 3 5 5 3 3 1 0 0                                               48-a 0.63 5 4 5 1 5 5 5 3 2 0 0                                               49-a 2.5 5 5 5 2 5 5 3 2 1 0 0                                                52-a 2.5 5 5 5 3 3 5 4 1 1 0 0                                                53-a 2.5 5 5 5 3 3 5 5 0 0 0 0                                                56-a 2.5 5 5 5 3 5 5 4 3 3 3 0                                                59-a 0.63 5 4 5 5 5 5 1 0 0 0 0                                               61-a 2.5 5 5 5 4 5 5 1 2 1 0 0                                                63-a 0.63 5 5 5 3 5 5 3 1 2 0 0                                               64-a 2.5 5 5 5 2 5 5 3 2 3 1 0                                                73-a 0.63 5 5 5 3 5 5 5 5 5 3 0                                               74-a 0.63 5 5 5 2 5 5 3 2 2 0 0                                                1-b 5 -- -- 4 -- 3 5 -- 0 0 0 --                                              3-b 5 -- -- 3 -- 2 4 -- 0 0 0 --                                              1-c 0.16 5 5 5 2 4 5 5 4 1 4 0                                                2-c 0.16 5 5 5 4 5 5 5 4 2 0 0                                                3-c 0.16 5 5 5 2 5 5 5 3 3 1 0                                                4-c 0.63 4 5 5 2 4 5 1 1 0 0 0                                                5-c 0.63 5 5 5 1 5 5 1 1 0 0 0                                                6-c 0.63 2 3 5 0 4 5 1 0 0 0 0                                                7-c 0.63 5 5 5 2 5 5 4 1 0 1 0                                                8-c 10 2 4 5 5 4 5 1 0 0 0 0                                                 11-c 0.63 5 5 5 2 5 5 3 2 1 0 0                                               12-c 0.16 5 5 5 2 5 5 4 3 0 0 0                                               13-c 0.16 5 5 5 4 5 5 4 3 3 0 0                                               14-c 0.63 5 5 5 0 5 5 2 0 0 0 0                                               15-c 0.63 5 5 5 3 5 5 2 1 0 0 0                                               16-c 0.63 5 5 5 4 5 5 4 4 3 0 0                                               17-c 0.63 5 5 5 3 5 5 2 0 0 0 0                                               18-c 0.16 5 5 5 3 5 5 5 2 0 0 0                                               20-c 0.63 0 0 3 3 5 5 0 0 0 0 0                                               23-c 0.63 4 3 5 5 5 5 5 1 2 0 0                                               24-c 0.16 5 5 1 2 5 5 4 1 1 0 0                                               26-c 0.63 5 5 4 2 5 5 5 3 5 3 0                                               35-c 0.16 5 5 5 3 5 5 5 5 4 0 0                                               36-c 0.16 5 5 5 3 5 5 5 4 4 0 0                                               37-c 0.16 5 5 5 4 5 5 5 5 5 4 1                                               38-c 0.63 5 5 5 3 5 5 5 5 2 0 1                                               39-c 0.63 5 5 5 3 5 5 4 4 3 1 0                                               40-c 0.16 5 5 5 4 5 5 5 5 5 2 2                                                2-d 2.5 4 5 5 5 4 5 0 0 0 0 0                                                 3-d 2.5 5 5 5 5 0 5 0 0 0 0 0                                                 5-d 2.5 3 5 5 5 3 5 3 0 0 0 0                                                 6-d 10 2 4 5 5 5 5 1 0 0 0 1                                                  9-d 10 3 5 5 5 5 5 3 1 1 0 0                                                  1-e 5 5 5 5 2 2 5 5 1 0 0 0                                                   2-e 2.5 3 3 2 1 0 2 0 0 0 0 0                                                 4-e 5 3 5 5 3 3 5 1 0 0 0 0                                                   2-f 10 4 5 5 5 5 5 4 0 1 0 0                                                  1-g 0.63 5 5 5 5 5 5 3 0 1 1 0                                                7-g 2.5 5 5 5 3 5 5 3 1 4 2 1                                                 9-g 2.5 5 5 5 5 5 5 0 0 0 0 0                                                11-g 0.63 5 5 5 3 5 5 3 2 1 1 0                                               12-g 2.5 5 4 5 3 5 5 1 1 1 0 0                                                13-g 2.5 5 3 5 3 5 5 1 0 1 0 0                                                14-g 2.5 4 4 5 3 5 5 0 0 0 0 0                                                15-g 2.5 5 4 5 3 5 5 1 1 2 0 0                                                16-g 2.5 5 4 5 3 5 5 3 3 4 0 0                                                17-g 0.63 5 5 5 5 5 5 3 1 3 0 0                                               18-g 0.63 5 5 5 5 5 5 4 2 2 0 0                                               19-g 2.5 4 5 5 2 5 5 4 3 3 1 0                   ______________________________________                                    

                                      TABLE 16                                    __________________________________________________________________________        Dose                                                                      No. (kg/ha)                                                                             A  B C D E F G a b c d e  f                                         __________________________________________________________________________     1-a                                                                              2.5   4  2 4 2 5 4 4 3 3 3 3 1  3                                          2-a                                                                              0.16  5  2 4 3 4 4 4 2 3 2 3 0  1                                             0.32  5  3 5 4 5 5 5 2 4 2 3 1  2                                             0.63  5  3 5 4 5 5 5 3 4 3 4 2  2                                          3-a                                                                              2.5   4  3 4 2 3 1 2 1 1 2 3 1  1                                          6-a                                                                              2.5   5  3 5 2 3 3 4 4 4 3 3 1  0                                          7-a                                                                              0.16  5  1 3 2 3 2 3 1 3 0 0 1  0                                             0.32  5  2 3 3 5 3 4 2 3 1 1 1  0                                             0.63  5  3 4 3 5 4 5 3 4 3 3 2  2                                          8-a                                                                              2.5   5  1 5 2 5 4 4 3 4 2 4 2  2                                         10-a                                                                              2.5   5  2 5 3 5 3 4 3 3 3 4 1  3                                         12-a                                                                              0.16  4  3 4 3 2 4 4 1 3 0 0 0  0                                             0.32  5  4 5 4 3 5 5 2 3 0 1 0  1                                             0.63  5  5 5 5 4 5 5 3 4 1 2 1  1                                         20-a                                                                              0.16  5  0 2 4 4 4 4 2 4 0 0 0  1                                             0.32  5  1 2 5 5 5 5 3 5 1 1 0  1                                             0.63  5  2 3 5 5 5 5 4 5 2 2 1  1                                         22-a                                                                              0.63  5  1 2 5 5 5 5 2 4 1 2 0  3                                         24-a                                                                              0.63  5  2 4 4 4 5 5 3 4 1 1 0  1                                         30-a                                                                              2.5   3  0 5 4 4 2 5 3 5 1 3 1  3                                         31-a                                                                              2.5   2  0 5 3 4 5 5 3 4 1 1 0  1                                         34-a                                                                              2.5   5  5 3 5 5 4 4 2 5 1 1 0  3                                         36-a                                                                              2.5   4  0 2 4 4 4 3 0 3 0 0 0  0                                         38-a                                                                              2.5   5  3 4 5 5 3 4 4 5 2 3 0  1                                         40-a                                                                              2.5   5  3 5 5 4 3 4 4 5 3 3 1  0                                         47-a                                                                              2.5   5  2 5 5 3 5 5 4 5 1 3 1  3                                         48-a                                                                              2.5   5  2 5 5 5 5 5 5 5 3 4 1  5                                         56-a                                                                              2.5   5  3 5 3 5 3 5 3 4 1 3 0  3                                         59-a                                                                              2.5   5  2 5 5 5 5 5 4 5 2 3 1  5                                         63-a                                                                              2.5   5  3 3 5 5 5 5 3 5 1 4 1  4                                         64-a                                                                              2.5   5  3 5 5 5 5 5 4 5 3 3 0  4                                         73-a                                                                              0.16  5  5 5 4 2 5 5 4 5 4 4 1  0                                         74-a                                                                              0.63  5  5 3 4 5 5 5 1 5 2 1 1  4                                          1-c                                                                              0.16  5  5 5 5 5 5 5 4 5 1 4 1  5                                          2-c                                                                              0.16  5  5 5 5 4 5 5 4 4 2 3 1  4                                          3-c                                                                              0.16  5  5 5 5 5 5 5 5 4 2 4 1  5                                          4-c                                                                              0.63  5  2 1 3 3 5 5 3 4 0 0 0  4                                          5-c                                                                              0.63  5  5 5 5 5 5 5 3 5 3 3 3  5                                          6-c                                                                              0.63  5  5 4 5 5 5 5 2 5 2 4 2  5                                          7-c                                                                              0.63  5  5 4 5 5 5 5 3 4 1 3 3  4                                          8-c                                                                              10    2  2 2 3 5 5 5 0 3 0 0 2  4                                         11-c                                                                              0.63  5  5 5 5 5 5 5 3 4 3 3 4  5                                         12-c                                                                              0.16  5  5 4 5 5 5 5 2 5 1 4 3  5                                         13-c                                                                              0.16  5  5 5 5 5 5 5 3 5 3 5 4  5                                         14-c                                                                              0.63  5  5 5 5 2 5 5 2 4 0 0 3  5                                         15-c                                                                              0.63  5  5 4 5 5 5 5 3 5 0 0 2  5                                         16-c                                                                              0.63  5  5 4 5 5 5 5 3 5 3 4 4  5                                         17-c                                                                              0.63  5  4 3 5 5 5 5 1 5 1 3 3  4                                         18-c                                                                              0.16  5  5 4 5 5 5 5 2 5 3 4 4  5                                         20-c                                                                              0.63  1  1 0 0 5 5 5 0 0 0 0 1  2                                         21-c                                                                              0.63  3  5 2 3 5 5 5 1 3 0 0 1  2                                         23-c                                                                              0.63  5  4 3 5 5 5 5 1 1 0 0 1  1                                         24-c                                                                              0.16  5  5 5 2 3 5 5 4 5 1 5 3  3                                         26-c                                                                              0.63  5  5 5 3 4 5 5 5 5 5 5 0  3                                         35-c                                                                              0.16  5  5 5 5 5 5 5 4 5 4 3 3  5                                         36-c                                                                              0.16  5  5 5 5 5 5 5 4 5 4 4 3  5                                         37-c                                                                              0.16  5  5 5 5 5 5 5 5 5 5 5 3  5                                         38-c                                                                              0.63  5  5 3 5 5 5 5 3 5 2 4 2  5                                         39-c                                                                              0.63  5  5 5 5 4 5 5 4 5 2 5 4  4                                         40-c                                                                              0.16  5  5 5 5 5 5 5 5 5 5 5 4  5                                          5-d                                                                              10    4  5 2 5 5 5 5 2 4 1 3 3  5                                          6-d                                                                              10    3  4 4 5 5 5 5 2 3 1 2 3  5                                          9-d                                                                              10    2  4 4 4 5 5 5 0 4 0 3 2  3                                          1-e                                                                              5     4  2 2 3 5 5 5 3 5 1 2 0  3                                          2-e                                                                              2.5   3  0 0 1 3 0 1 1 0 0 0 0  1                                          4-e                                                                              5     2  0 4 4 5 5 3 2 3 0 0 0  4                                          2-f                                                                              10    3  0 2 2 5 5 4 1 3 0 2 0  3                                          1-g                                                                              2.5   5  4 --                                                                              5 5 5 5 4 4 2 4 1  4                                          7-g                                                                              2.5   2  3 5 5 5 5 5 1 5 2 4 3  5                                          9-g                                                                              2.5   2  3 4 5 5 4 5 0 3 1 5 2  5                                         11-g                                                                              2.5   5  5 3 5 5 5 5 2 5 4 4 3  4                                         12-g                                                                              2.5   4  3 3 3 5 5 5 0 4 1 4 1  3                                         13-g                                                                              2.5   4  2 3 3 5 5 5 0 4 1 4 1  3                                         14-g                                                                              2.5   3  1 3 3 5 5 5 0 4 1 4 1  3                                         15-g                                                                              2.5   4  3 5 5 5 5 5 1 5 3 4 2  4                                         16-g                                                                              2.5   5  3 5 5 5 5 5 2 5 3 5 2  4                                         17-g                                                                              2.5   5  5 5 4 5 5 5 5 5 5 5 1  3                                         18-g                                                                              2.5   5  5 5 4 5 5 5 5 5 5 5 3  5                                         19-g                                                                              2.5   3  2 2 3 5 5 3 1 4 2 3 2  3                                         __________________________________________________________________________

                  TABLE 17                                                        ______________________________________                                              Dose                                                                    No.   (kg/ha)  A       H   I     J   K     L   a                              ______________________________________                                        74-a  2.5      5       4   4     4   5     4   0                               1-b  4        4       --  5     5   5     --  0                               1-c  0.64     5       5   4     5   5     5   0                               7-c  2.5      5       0   4     4   4     4   0                              13-c  0.64     5       4   5     4   5     5   0                              50-c  0.64     5       4   5     5   5     4   0                              53-c  0.16     5       0   4     5   4     2   0                              54-c  0.16     5       2   4     4   5     5   0                              ______________________________________                                    

TEST EXAMPLE 4: Test-2 on the herbicidal effects in soil treatment

A plastic box having a length of 21 cm, a width of 13 cm and a depth of7 cm was filled with a sterilized diluvial soil, and seeds ofEchinochloa crus-galli, Setaria viridis, Avena fatua, Alopecurusmyosuroides, Abutilon theophrasti, Xanthium strumarium, Amaranthusviridis, Ipomoea spp., Veronica persica, Stellaria media, Zea mays,Oryza sativa, Oryza sativa, Glycine max, Gossypium spp., Triticumaestivum and Beta vulgaris were spot-wisely sown, and the soil wascovered thereon in a thickness of about 1.5 cm, and then a herbicidesolution was applied onto the surface of the soil uniformly so that theactive ingredient was distributed at a predetermined concentration. Theherbicide solution was prepared by diluting a wettable powder preparedin accordance with the foregoing Formulation Examples with water andapplied onto the entire soil surface by a small spray. Three weeks afterthe application of the herbicidal solution, the herbicidal effectsagainst each weed and the phytotoxicities against each crop plant werevisually determined on the basis of the following standard ratings. Theresults are shown in Table 18.

Some of the compounds of the present invention show selectivity forcertain crop plants.

Standard ratings:

5: Growth control rate of more than 90% (almost completely withered)

4: Growth control rate of from 70 to 90%

3: Growth control rate of from 40 to 70%

2: Growth control rate of from 20 to 40%

1: Growth control rate of from 5 to 20%

0: Growth control rate of less than 5% (almost non-effective)

TEST EXAMPLE 5: Test-2 on the herbicidal effects in foliage treatment

A plastic box having a length of 21 cm, a width of 13 cm and a depth of7 cm was filled with a sterilized diluvial soil, and seeds ofEchinochloa crus-galli, Setaria viridis, Avena fatua, Alopecurusmyosuroides, Abutilon theophrasti, Xanthium strumarium, Amaranthusviridis, Ipomoea spp., Veronica persica, Stellaria media, Zea mays,Oryza sativa, Glycine max, Gossypium spp., Triticum aestivum and Betavulgaris were spot-wisely sown and the soil was covered thereon in athickness of about 1.5 cm. When the various weeds and crop plants grewto the 2 or 3 leaf stage, a herbicidal solution was uniformly sprayed onthe foliages so that the active ingredient was applied in apredetermined concentration. The herbicidal solution was prepared bydiluting a wettable powder prepared in accordance with the aboveFormulation Examples with water and applied onto the entire surface ofthe foliages of the weeds and the crop plants by a small spray. Threeweeks after the application of the herbicide solution, the herbicidaleffects against each weed and the phytotoxicities against each cropplant were visually determined on the basis of the standard ratingsdescribed in Test Example 4. The results are shown in Table 19.

TEST EXAMPLE 6: Test-2 on the herbicidal effects during the growingstage in irrigation treatment

Into a Wagner pot of 1/5000a, alluvial soil was put, and then water wasintroduced and mixed to form an irrigated state with a water depth of 4cm. Seeds of Echinochloa crus-galli, Scirpus juncoides, Monochoriavaginalis and Rotala indica were sown in the above pot. The pot wasplaced in a greenhouse at a temperature of from 25° to 30° C., and theplants were cultured. When Echinochloa crus-galli, Scirpus juncoides,Monochoria vaginalis and Rotala indica reached 1 to 2 leaf stage, adiluted solution of the herbicide was dropwise applied to the watersurface by a measuring pipette, so that the dose would be apredetermined level. Three weeks after the dropwise application of theherbicide, the herbicidal effects to various weeds were visuallydetermined on the basis of the standard ratings described in TestExample 4. The results are shown in Table 20.

In Tables 18, 19 and 20, Nos. correspond to Compound Nos. in theExamples, and symbols have the following meanings.

A: Echinochloa crus-galli (barnyardgrass)

B: Setaria viridis (green foxtail)

C: Avena fatua (wild oat)

D: Alopecurus myosuroides (black grass)

E: Abutilon theophrasti (velvetleaf)

F: Xanthium strumarium (common cocklebur)

G: Amaranthus viridis (slender amaranth)

H: Ipomoea spp. (mornigglory)

I: Veronica persica (Persian speedwell)

J: Stellaria media (common chickweed)

a: Zea mays (corn)

b: Oryza sativa (rice)

c: Glycine max (soybean)

d: Gossypium spp. (cotton)

e: Triticum aestivum (wheat)

f: Beta vulgaris (sugar beet)

                                      TABLE 18                                    __________________________________________________________________________       Dose                                                                       No.                                                                              (kg/ha)                                                                            A B C D E F G H I J a b c d e f                                       __________________________________________________________________________    41-c                                                                             0.16 5 5 3 5 5 5 5 4 2 5 4 5 3 0 3 4                                       43-c                                                                             0.63 5 5 3 5 3 1 5 3 5 5 5 5 1 0 4 4                                       44-c                                                                             0.63 5 5 5 5 5 3 5 5 5 5 5 5 4 0 4 4                                       49-c                                                                             0.63 5 5 2 5 5 2 5 5 5 5 5 5 0 2 2 5                                       50-c                                                                             0.63 5 5 4 5 5 2 5 5 5 5 5 5 1 1 3 5                                       51-c                                                                             0.16 5 5 4 5 5 5 5 5 5 5 5 5 3 1 2 4                                       52-c                                                                             0.63 5 5 5 5 2 5 5 5 5 5 5 5 3 3 4 4                                       53-c                                                                             0.16 5 5 5 5 2 5 5 5 5 5 4 5 0 0 4 5                                       54-c                                                                             0.63 5 5 5 5 5 5 5 5 5 5 5 5 3 1 4 5                                       55-c                                                                             0.63 5 5 5 5 4 5 5 5 5 5 5 5 1 0 5 5                                       56-c                                                                             0.63 5 5 5 5 5 5 5 5 5 5 5 5 3 1 5 5                                       20-g                                                                             0.63 5 5 3 5 5 2 5 3 5 5 4 4 2 0 2 5                                       __________________________________________________________________________

                                      TABLE 19                                    __________________________________________________________________________       Dose                                                                       No.                                                                              (kg/ha)                                                                            A B C D E F G H I J a b c d e f                                       __________________________________________________________________________    41-c                                                                             0.16 5 5 4 5 5 5 5 5 1 5 5 3 4 2 2 5                                       43-c                                                                             0.63 5 5 4 5 5 5 5 3 2 5 5 3 0 1 2 5                                       44-c                                                                             0.63 5 5 5 5 5 5 5 5 3 5 5 4 4 3 3 5                                       49-c                                                                             0.63 5 5 2 5 5 5 5 5 5 5 5 2 4 2 1 5                                       50-c                                                                             0.63 5 5 3 5 5 5 5 5 4 5 5 3 4 3 1 5                                       51-c                                                                             0.16 5 5 3 4 5 5 5 5 5 5 5 4 5 1 2 5                                       52-c                                                                             0.63 5 5 5 5 5 5 5 4 2 5 5 4 4 1 4 5                                       53-c                                                                             0.16 5 5 5 5 5 5 5 5 5 5 5 5 5 3 4 5                                       54-c                                                                             0.16 5 5 5 5 5 5 5 5 5 5 5 5 5 3 3 5                                       55-c                                                                             0.16 5 5 5 5 5 5 5 3 5 5 5 5 5 1 5 5                                       56-c                                                                             0.16 5 5 5 5 5 5 5 2 5 5 5 5 5 1 5 5                                       20-g                                                                             0.63 5 5 5 5 5 5 5 4 5 5 5 5 5 3 4 5                                       __________________________________________________________________________

                  TABLE 20                                                        ______________________________________                                                Dose                                                                  No.     (kg/ha)      A     H       I   J                                      ______________________________________                                        50-c    0.64         5     4       4   4                                      53-c    0.16         5     3       4   2                                      54-c    0.16         5     4       4   4                                      ______________________________________                                    

INDUSTRIAL APPLICABILITY

Iminosulfonylurea derivatives of the formula (1) of the presentinvention can be used safely to important crop plants, and they arecompounds showing high herbicidal effects against many weeds and thususeful as active ingredients of herbicides.

We claim:
 1. An iminosulfonylurea derivative of formula (I) or its salt:##STR787## wherein Q is ##STR788## R^(a1) is a C₁₋₈ alkyl group, a C₃₋₇cycloalkyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ cycloalkylgroup, a C₃₋₇ cycloalkenyl group, a C₁₋₆ alkyl group substituted by aC₃₋₇ cycloalkenyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynyl group, aC₁₋₆ alkyl group substituted by a C₁₋₆ alkoxy group, a C₁₋₆ alkyl groupsubstituted by a C₂₋₆ alkenyloxy group, a C₁₋₆ alkyl group substitutedby a C₂₋₆ alkynyloxy group, a C₁₋₆ alkyl group substituted by a mono-,di- or poly-halogeno C₁₋₆ alkoxy group, a C₁₋₆ alkyl group substitutedby a mono-, di- or poly-halogeno C₂₋₆ alkenyloxy group, a C₁₋₆ alkylgroup substituted by a mono-, di- or poly-halogeno C₂₋₆ alkynyloxygroup, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylthio group, a C₁₋ 6alkyl group substituted by a C₁₋₆ alkylsulfinyl group, a C₁₋₆ alkylgroup substituted by a C₁₋₆ alkylsulfonyl group, a mono-, di- orpoly-halogeno C₁₋₈ alkyl group, a mono-, di- or poly-halogeno C₂₋₈alkenyl group, a mono-, di- or poly-halogeno C₂₋₈ alkynyl group, a C₁₋₆alkyl group substituted by a cyano group, a C₂₋₆ alkenyl groupsubstituted by a cyano group, a C₂₋₆ alkynyl group substituted by acyano group, a C₁₋₆ alkyl group substituted by a nitro group, a C₂₋₆alkenyl group substituted by a nitro group, a C₂₋₆ alkynyl groupsubstituted by a nitro group, a C₁₋₆ alkyl group substituted by a C₂₋₇alkoxycarbonyl group, a C₂₋₆ alkenyl group substituted by a C₂₋₇alkoxycarbonyl group, a C₂₋₆ alkynyl group substituted by a C₂₋₇alkoxycarbonyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a mono-, di- orpoly-halogeno C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substitutedby a C₃₋₇ alkenylcarbonyl group, a C₁₋₆ alkyl group substituted by aC₃₋₇ alkynylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₂₋₅alkylcarbonyl group substituted by a C₁₋₄ alkoxy group, a C₁₋₆ alkylgroup substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄alkylthio group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonylgroup substituted by a C₁₋₄ alkylsulfinyl group, a C₁₋₆ alkyl groupsubstituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄alkylsulfonyl group, a C₂₋₆ alkenyl group substituted by a C₂₋₇alkylcarbonyl group, a C₂₋₆ alkynyl group substituted by a C₂₋₇alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆alkylsulfamoyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆alkoxysulfamoyl group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃alkyl)sulfamoyl group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃alkyl)-N-(C₁₋₃ alkoxy)sulfamoyl group, a C₁₋₆ alkyl group substituted bya C₂₋₇ alkylcarbamoyl group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃alkyl)carbamoyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇alkoxycarbamoyl group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃alkyl)-N-(C₁₋₃ alkoxy)carbamoyl group, a C₁₋₆ alkyl group substituted bya C₁₋₆ alkylamino group, a C₁₋₆ alkyl group substituted by a C₁₋₆alkoxyamino group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃alkyl)-N-(C₁₋₃ alkoxy)amino group, a C₁₋₆ alkyl group substituted by anN-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆ alkyl)amino group, a C₁₋₆ alkyl groupsubstituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆ alkoxy)amino group, aC₁₋₆ alkyl group substituted by an N-(C₁₋₆ alkylsulfonyl)-N-(C₁₋₆alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₆alkylsulfonyl)-N-(C₁₋₆ alkoxy)amino group, a phenyl group (provided thatsuch a phenyl group may be substituted by one or more substituentsselected from the group consisting of a halogen atom, a trifluoromethylgroup, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenyl group(provided that such a phenyl group may be substituted by one or moresubstituents selected from the group consisting of a halogen atom, atrifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxygroup and a C₂₋₇ alkoxycarbonyl group), a C₂₋₇ alkenyl group substitutedby a phenyl group (provided that such a phenyl group may be substitutedby one or more substituents selected from the group consisting of ahalogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkylgroup, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₂₋₆alkynyl group substituted by a phenyl group (provided that such a phenylgroup may be substituted by one or more substituents selected from thegroup consisting of a halogen atom, a trifluoromethyl group, a nitrogroup, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonylgroup), a C₁₋₆ alkyl group substituted by a phenoxy group (provided thatsuch a phenoxy group may be substituted by one or more substituentsselected from the group consisting of a halogen atom, a trifluoromethylgroup, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylthiogroup (provided that such a phenylthio group may be substituted by oneor more substituents selected from the group consisting of a halogenatom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl groupsubstituted by a phenylsulfinyl group (provided that such aphenylsulfinyl group may be substituted by one or more substituentsselected from the group consisting of a halogen atom, a trifluoromethylgroup, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by aphenylsulfonyl group (provided that such a phenylsulfonyl group may besubstituted by one or more substituents selected from the groupconsisting of a halogen atom, a trifluoromethyl group, a nitro group, aC₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),a C₁₋₆ alkyl group substituted by a benzyloxy group (provided that thephenyl group of such a benzyloxy group may be substituted by one or moresubstituents selected from the group consisting of a halogen atom, atrifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxygroup and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substitutedby a benzylthio group (provided that the phenyl group of such abenzylthio group may be substituted by one or more substituents selectedfrom the group consisting of a halogen atom, a trifluoromethyl group, anitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by abenzylsulfinyl group (provided that the phenyl group of such abenzylsulfinyl group may be substituted by one or more substituentsselected from the group consisting of a halogen atom, a trifluoromethylgroup, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by abenzylsulfonyl group (provided that the phenyl group of such abenzylsulfonyl group may be substituted by one or more substituentsselected from the group consisting of a halogen atom, a trifluoromethylgroup, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by aphenylcarbonyl group (provided that such a phenylcarbonyl group may besubstituted by one or more substituents selected from the groupconsisting of a halogen atom, a trifluoromethyl group, a nitro group, aC₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),a C₁₋₆ alkyl group substituted by a benzylcarbonyl group (provided thatthe phenyl group of such a benzylcarbonyl group may be substituted byone or more substituents selected from the group consisting of a halogenatom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl groupsubstituted by an amino group substituted by a C₁₋₄ alkylsulfonyl group,or a C₁₋₆ alkyl group substituted by an amino group substituted by aC₂₋₄ alkylcarbonyl group,each of R^(a2) and R^(a3) which are independentof each other, is a hydrogen atom, a C₁₋₆ alkyl group, a mono-, di- orpoly-halogeno C₁₋₆ alkyl group, a C₁₋₆ alkoxy group, a mono-, di orpoly-halogeno C₁₋₆ alkoxy group, a C₁₋₆ alkylthio group, a C₁₋₆alkylsulfinyl group, a C₁₋₆ alkylsulfonyl group, a C₂₋₇ alkoxycarbonylgroup, a C₂₋₇ alkylcarbonyl group, a halogen atom, a nitro group, acyano group, or a phenyl group (provided that such a phenyl group may besubstituted by one or more substituents selected from the groupconsisting of a halogen atom, a trifluoromethyl group, a nitro group, aC₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),each of R^(a4) and R^(a5) which are independent of each other, is ahydrogen atom, a C₁₋₈ alkyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynylgroup, or a phenyl group (provided that such a phenyl group may besubstituted by one or more substituents selected from the groupconsisting of a halogen atom, a trifluoromethyl group, a nitro group, aC₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),R^(a6) is a C₁₋₈ alkyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynyl groupor a phenyl group (provided that such a phenyl group may be substitutedby one or more substituents selected from the group consisting of ahalogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkylgroup, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), R^(b1) is aC₁₋₈ alkyl group, a C₃₋₇ cycloalkyl group, a C₁₋₆ alkyl groupsubstituted by a C₃₋₇ cycloalkyl group, a C₃₋₇ cycloalkenyl group, aC₁₋₆ alkyl group substituted by a C₃₋₇ cycloalkenyl group, a C₂₋₈alkenyl group, a C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by aC₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkenyloxygroup, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkynyloxy group, a C₁₋₆alkyl group substituted by a mono-, di or poly-halogeno C₁₋₆ alkoxygroup, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogenoC₂₋₆ alkenyloxy group, a C₁₋₆ alkyl group substituted by a mono-, di- orpoly-halogeno C₂₋₆ alkynyloxy group, a C₁₋₆ alkyl group substituted by aC₁₋₆ alkylthio group, a C₁₋₆ alkyl group substituted by a C₁₋₆alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆alkylsulfonyl group, a mono-, di- or poly-halogeno C₁₋₈ alkyl group, amono-, di- or poly-halogeno C₂₋₈ alkenyl group, a mono-, di- orpoly-halogeno C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by acyano group, a C₂₋₆ alkenyl group substituted by a cyano group, a C₂₋₆alkynyl group substituted by a cyano group, a C₁₋₆ alkyl groupsubstituted by a nitro group, a C₂₋₆ alkenyl group substituted by anitro group, a C₂₋₆ alkynyl group substituted by a nitro group, a C₁₋₆alkyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkenylgroup substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkynyl groupsubstituted by a C₂₋₇ alkoxycarbonyl group, a C₁₋₆ alkyl groupsubstituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl groupsubstituted by a mono-, di- or poly-halogeno C.sub. 2-7 alkylcarbonylgroup, a C₁₋₆ alkyl group substituted by a C₃₋₇ alkenylcarbonyl group, aC₁₋₆ alkyl group substituted by a C₃₋₇ alkynylcarbonyl group, a C₁₋₆alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by aC₁₋₄ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₅alkylcarbonyl group substituted by a C₁₋₄ alkylthio group, a C₁₋₆ alkylgroup substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₂₋₅alkylcarbonyl group substituted by a C₁₋₄ alkylsulfonyl group, a C₂₋₆alkenyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₂₋₆ alkynylgroup substituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl groupsubstituted by a C₁₋₆ alkylsulfamoyl group, a C₁₋₆ alkyl groupsubstituted by a C₁₋₆ alkoxysulfamoyl group, a C₁₋₆ alkyl groupsubstituted by a di(C₁₋₃ alkyl)sulfamoyl group, a C₁₋₆ alkyl groupsubstituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)sulfamoyl group, a C₁₋₆alkyl group substituted by a C₂₋₇ alkylcarbamoyl group, a C₁₋₆ alkylgroup substituted by a di(C₁₋₃ alkyl)carbamoyl group, a C₁₋₆ alkyl groupsubstituted by a C₂₋₇ alkoxycarbamoyl group, a C₁₋₆ alkyl groupsubstituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)carbamoyl group, a C₁₋₆alkyl group substituted by a C₁₋₆ alkylamino group, a C₁₋₆ alkyl groupsubstituted by a C₁₋₆ alkoxyamino group, a C₁₋₆ alkyl group substitutedby a di(C₁₋₃ alkyl)amino group, a C₁₋₆ alkyl group substituted by anN-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)amino group, a C₁₋₆ alkyl groupsubstituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆ alkyl)amino group, aC₁₋₆ alkyl group substituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆alkoxy)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₆alkylsulfonyl)-N-(C₁₋₆ alkyl)amino group, a C₁₋₆ alkyl group substitutedby an N-(C₁₋₆ alkylsulfonyl)-N-(C₁₋₆ alkoxy)amino group, a phenyl group(provided that such a phenyl group may be substituted by one or moresubstituents selected from the group consisting of a halogen atom, atrifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxygroup and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substitutedby a phenyl group (provided that such a phenyl group may be substitutedby one or more substituents selected from the group consisting of ahalogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkylgroup, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₂₋₇alkenyl group substituted by a phenyl group (provided that such a phenylgroup may be substituted by one or more substituents selected from thegroup consisting of a halogen atom, a trifluoromethyl group, a nitrogroup, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonylgroup), a C₂₋₆ alkynyl group substituted by a phenyl group (providedthat such a phenyl group may be substituted by one or more substituentsselected from the group consisting of a halogen atom, a trifluoromethylgroup, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenoxy group(provided that such a phenoxy group may be substituted by one or moresubstituents selected from the group consisting of a halogen atom, atrifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxygroup and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substitutedby a phenylthio group (provided that such a phenylthio group may besubstituted by one or more substituents selected from the groupconsisting of a halogen atom, a trifluoromethyl group, a nitro group, aC₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),a C₁₋₆ alkyl group substituted by a phenylsulfinyl group (provided thatsuch a phenylsulfinyl group may be substituted by one or moresubstituents selected from the group consisting of a halogen atom, atrifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxygroup and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substitutedby a phenylsulfonyl group (provided that such a phenylsulfonyl group maybe substituted by one or more substituents selected from the groupconsisting of a halogen atom, a trifluoromethyl group, a nitro group, aC₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),a C₁₋₆ alkyl group substituted by a benzyloxy group (provided that thephenyl group of such a benzyloxy group may be substituted by one or moresubstituents selected from the group consisting of a halogen atom, atrifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxygroup and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substitutedby a benzylthio group (provided that the phenyl group of such abenzylthio group may be substituted by one or more substituents selectedfrom the group consisting of a halogen atom, a trifluoromethyl group, anitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by abenzylsulfinyl group (provided that the phenyl group of such abenzylsulfinyl group may be substituted by one or more substituentsselected from the group consisting of a halogen atom, a trifluoromethylgroup, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by abenzylsulfonyl group (provided that the phenyl group of such abenzylsulfonyl group may be substituted by one or more substituentsselected from the group consisting of a halogen atom, a trifluoromethylgroup, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by aphenylcarbonyl group (provided that such a phenylcarbonyl group may besubstituted by one or more substituents selected from the groupconsisting of a halogen atom, a trifluoromethyl group, a nitro group, aC₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),a C₁₋₆ alkyl group substituted by a benzylcarbonyl group (provided thatthe phenyl group of such a benzylcarbonyl group may be substituted byone or more substituents selected from the group consisting of a halogenatom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl groupsubstituted by an amino group substituted by a C₁₋₄ alkylsulfonyl group,or a C₁₋₆ alkyl group substituted by an amino group substituted by aC₂₋₄ alkylcarbonyl group, R^(b2) is a hydrogen atom, a C₁₋₆ alkyl group,a mono-, di- or poly-halogeno C₁₋₆ alkyl group, a C₁₋₆ alkoxy group, amono-, di- or poly-halogeno C₁₋₆ alkoxy group, a C₁₋₆ alkylthio group, aC₁₋₆ alkylsulfinyl group, a C₁₋₆ alkylsulfonyl group, a C₂₋₇alkoxycarbonyl group, a C₂₋₇ alkylcarbonyl group, a halogen atom, anitro group, a cyano group, or a phenyl group (provided that such aphenyl group may be substituted by one or more substituents selectedfrom the group consisting of a halogen atom, a trifluoromethyl group, anitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), R^(b3) is a C₁₋₆ alkyl group, a C₂₋₆ alkenylgroup or a C₂₋₆ alkynyl group, R^(b4) is a hydrogen atom, or a C₁₋₆alkyl group, R^(b5) is a hydrogen atom, or a C₁₋₆ alkyl group, R^(c1) isa C₁₋₈ alkyl group, a C₃₋₇ cycloalkyl group, a C₁₋₆ alkyl groupsubstituted by a C₃₋₇ cycloalkyl group, a C₃₋₇ cycloalkenyl group, aC₁₋₆ alkyl group substituted by a C₃₋₇ cycloalkenyl group, a C₂₋₈alkenyl group, a C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by aC₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkenyloxygroup, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkynyloxy group, a C₁₋₆alkyl group substituted by a mono-, di- or poly-halogeno C₁₋₆ alkoxygroup, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogenoC₂₋₆ alkenyloxy group, a C₁₋₆ alkyl group substituted by a mono-, di- orpoly-halogeno C₂₋₆ alkynyloxy group, a C₁₋₆ alkyl group substituted by aC₁₋₆ alkylthio group, a C₁₋₆ alkyl group substituted by a C₁₋₆alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆alkylsulfonyl group, a mono-, di- or poly-halogeno C₁₋₈ alkyl group, amono-, di- or poly-halogeno C₂₋₈ alkenyl group, a mono-, di- orpoly-halogeno C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by acyano group, a C₂₋₆ alkenyl group substituted by a cyano group, a C₂₋₆alkynyl group substituted by a cyano group, a C₁₋₆ alkyl groupsubstituted by a nitro group, a C₂₋₆ alkenyl group substituted by anitro group, a C₂₋₆ alkynyl group substituted by a nitro group, a C₁₋₆alkyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkenylgroup substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkynyl groupsubstituted by a C₂₋₇ alkoxycarbonyl group, a C₁₋₆ alkyl groupsubstituted by a C₂₋₇ alkylcarbonyl group, a C.sub. 1-6 alkyl groupsubstituted by a mono-, di- or poly-halogeno C₂₋₇ alkylcarbonyl group, aC₁₋₆ alkyl group substituted by a C₃₋₇ alkenylcarbonyl group, a C₁₋₆alkyl group substituted by a C₃₋₇ alkynylcarbonyl group, a C₁₋₆ alkylgroup substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonylgroup substituted by a C₁₋₄ alkylthio group, a C₁₋₆ alkyl groupsubstituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₂₋₅alkylcarbonyl group substituted by a C₁₋₄ alkylsulfonyl group, a C₂₋₆alkenyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₂₋₆ alkynylgroup substituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl groupsubstituted by a C₁₋₆ alkylsulfamoyl group, a C₁₋₆ alkyl groupsubstituted by a C₁₋₆ alkoxysulfamoyl group, a C₁₋₆ alkyl groupsubstituted by a di(C₁₋₃ alkyl)sulfamoyl group, a C₁₋₆ alkyl groupsubstituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)sulfamoyl group, a C₁₋₆alkyl group substituted by a C₂₋₇ alkylcarbamoyl group, a C₁₋₆ alkylgroup substituted by a di(C₁₋₃ alkyl)carbamoyl group, a C₁₋₆ alkyl groupsubstituted by a C₂₋₇ alkoxycarbamoyl group, a C₁₋₆ alkyl groupsubstituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)carbamoyl group, a C₁₋₆alkyl group substituted by a C₁₋₆ alkylamino group, a C₁₋₆ alkyl groupsubstituted by a C₁₋₆ alkoxyamino group, a C₁₋₆ alkyl group substitutedby a di(C₁₋₃ alkyl)amino group, a C₁₋₆ alkyl group substituted by anN-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)amino group, a C₁₋₆ alkyl groupsubstituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆ alkyl)amino group, aC₁₋₆ alkyl group substituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆alkoxy)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₆alkylsulfonyl)-N-(C₁₋₆ alkyl)amino group, a C₁₋₆ alkyl group substitutedby an N-(C₁₋₆ alkylsulfonyl)-N-(C₁₋₆ alkoxy)amino group, a phenyl group(provided that such a phenyl group may be substituted by one or moresubstituents selected from the group consisting of a halogen atom, atrifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxygroup and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substitutedby a phenyl group (provided that such a phenyl group may be substitutedby one or more substituents selected from the group consisting of ahalogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkylgroup, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₂₋₇alkenyl group substituted by a phenyl group (provided that such a phenylgroup may be substituted by one or more substituents selected from thegroup consisting of a halogen atom, a trifluoromethyl group, a nitrogroup, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonylgroup), a C₂₋₆ alkynyl group substituted by a phenyl group (providedthat such a phenyl group may be substituted by one or more substituentsselected from the group consisting of a halogen atom, a trifluoromethylgroup, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenoxy group(provided that such a phenoxy group may be substituted by one or moresubstituents selected from the group consisting of a halogen atom, atrifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxygroup and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substitutedby a phenylthio group (provided that such a phenylthio group may besubstituted by one or more substituents selected from the groupconsisting of a halogen atom, a trifluoromethyl group, a nitro group, aC₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),a C₁₋₆ alkyl group substituted by a phenylsulfinyl group (provided thatsuch a phenylsulfinyl group may be substituted by one or moresubstituents selected from the group consisting of a halogen atom, atrifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxygroup and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substitutedby a phenylsulfonyl group (provided that such a phenylsulfonyl group maybe substituted by one or more substituents selected from the groupconsisting of a halogen atom, a trifluoromethyl group, a nitro group, aC₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),a C₁₋₆ alkyl group substituted by a benzyloxy group (provided that thephenyl group of such a benzyloxy group may be substituted by one or moresubstituents selected from the group consisting of a halogen atom, atrifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxygroup and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substitutedby a benzylthio group (provided that the phenyl group of such abenzylthio group may be substituted by one or more substituents selectedfrom the group consisting of a halogen atom, a trifluoromethyl group, anitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by abenzylsulfinyl group (provided that the phenyl group of such abenzylsulfinyl group may be substituted by one or more substituentsselected from the group consisting of a halogen atom, a trifluoromethylgroup, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by abenzylsulfonyl group (provided that the phenyl group of such abenzylsulfonyl group may be substituted by one or more substituentsselected from the group consisting of a halogen atom, a trifluoromethylgroup, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by aphenylcarbonyl group (provided that such a phenylcarbonyl group may besubstituted by one or more substituents selected from the groupconsisting of a halogen atom, a trifluoromethyl group, a nitro group, aC₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),a C₁₋₆ alkyl group substituted by a benzylcarbonyl group (provided thatthe phenyl group of such a benzylcarbonyl group may be substituted byone or more substituents selected from the group consisting of a halogenatom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl groupsubstituted by an amino group substituted by a C₁₋₄ alkylsulfonyl group,or a C₁₋₆ alkyl group substituted by an amino group substituted by aC₂₋₄ alkylcarbonyl group, each of R^(c2) and R^(c3) which areindependent of one another, is a hydrogen atom, a C₁₋₈ alkyl group, aC₂₋₈ alkenyl group, a C₂₋₈ alkynyl group, or a phenyl group (providedthat such a phenyl group may be substituted by one or more substituentsselected from the group consisting of a halogen atom, a trifluoromethylgroup, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), each of R^(c7) and R^(c8) which are independentof one another, is a hydrogen atom, a C₁₋₆ alkyl group, a mono-, di- orpoly-halogeno C₁₋₆ alkyl group, a C₁₋₆ alkoxy group, a mono, di- orpoly-halogeno C₁₋₆ alkoxy group, a C₁₋₆ alkylthio group, a C₁₋₆alkylsulfinyl group, a C₁₋₆ alkylsulfonyl group, a C₂₋₇ alkoxycarbonylgroup, a C₂₋₇ alkylcarbonyl group, a halogen atom, a nitro group, acyano group, or a phenyl group (provided that such a phenyl group may besubstituted by one or more substituents selected from the groupconsisting of a halogen atom, a trifluoromethyl group, a nitro group, aC₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),R^(d1) is a C₁₋₈ alkyl group, a C₃₋₇ cycloalkyl group, a C₁₋₆ alkylgroup substituted by a C₃₋₇ cycloalkyl group, a C₃₋₇ cycloalkenyl group,a C₁₋₆ alkyl group substituted by a C₃₋₇ cycloalkenyl group, a C₂₋₈alkenyl group, a C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by aC₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkenyloxygroup, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkynyloxy group, a C₁₋₆alkyl group substituted by a mono-, di or poly-halogeno C₁₋₆ alkoxygroup, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogenoC₂₋₆ alkenyloxy group, a C₁₋₆ alkyl group substituted by a mono-, di- orpoly-halogeno C₂₋₆ alkynyloxy group, a C₁₋₆ alkyl group substituted by aC₁₋₆ alkylthio group, a C₁₋₆ alkyl group substituted by a C₁₋₆alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆alkylsulfonyl group, a mono-, di- or poly-halogeno C₁₋₈ alkyl group, amono-, di- or poly-halogeno C₂₋₈ alkenyl group, a mono-, di- orpoly-halogeno C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by acyano group, a C₂₋₆ alkenyl group substituted by a cyano group, a C₂₋₆alkynyl group substituted by a cyano group, a C₁₋₆ alkyl groupsubstituted by a nitro group, a C₂₋₆ alkenyl group substituted by anitro group, a C₂₋₆ alkynyl group substituted by a nitro group, a C₁₋₆alkyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkenylgroup substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkynyl groupsubstituted by a C₂₋₇ alkoxycarbonyl group, a C₁₋₆ alkyl groupsubstituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl groupsubstituted by a mono-, di- or poly-halogeno C₂₋₇ alkylcarbonyl group, aC₁₋₆ alkyl group substituted by a C₃₋₇ alkenylcarbonyl group, a C₁₋₆alkyl group substituted by a C₃₋₇ alkynylcarbonyl group, a C₁₋₆ alkylgroup substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonylgroup substituted by a C₁₋₄ alkylthio group, a C₁₋₆ alkyl groupsubstituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₂₋₅alkylcarbonyl group substituted by a C₁₋₄ alkylsulfonyl group, a C₂₋₆alkenyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₂₋₆ alkynylgroup substituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl groupsubstituted by a C₁₋₆ alkylsulfamoyl group, a C₁₋₆ alkyl groupsubstituted by a C₁₋₆ alkoxysulfamoyl group, a C₁₋₆ alkyl groupsubstituted by a di(C₁₋₃ alkyl)sulfamoyl group, a C₁₋₆ alkyl groupsubstituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)sulfamoyl group, a C₁₋₆alkyl group substituted by a C₂₋₇ alkylcarbamoyl group, a C₁₋₆ alkylgroup substituted by a di(C₁₋₃ alkyl)carbamoyl group, a C₁₋₆ alkyl groupsubstituted by a C₂₋₇ alkoxycarbamoyl group, a C₁₋₆ alkyl groupsubstituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)carbamoyl group, a C₁₋₆alkyl group substituted by a C₁₋₆ alkylamino group, a C₁₋₆ alkyl groupsubstituted by a C₁₋₆ alkoxyamino group, a C₁₋₆ alkyl group substitutedby a di(C₁₋₃ alkyl)amino group, a C₁₋₆ alkyl group substituted by anN-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)amino group, a C₁₋₆ alkyl groupsubstituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆ alkyl)amino group, aC₁₋₆ alkyl group substituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆alkoxy)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₆alkylsulfonyl)-N-(C.sub. 1-6 alkyl)amino group, a C₁₋₆ alkyl groupsubstituted by an N-(C₁₋₆ alkylsulfonyl)-N-(C₁₋₆ alkoxy)amino group, aphenyl group (provided that such a phenyl group may be substituted byone or more substituents selected from the group consisting of a halogenatom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl groupsubstituted by a phenyl group (provided that such a phenyl group may besubstituted by one or more substituents selected from the groupconsisting of a halogen atom, a trifluoromethyl group, a nitro group, aC₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),a C₂₋₇ alkenyl group substituted by a phenyl group (provided that such aphenyl group may be substituted by one or more substituents selectedfrom the group consisting of a halogen atom, a trifluoromethyl group, anitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₂₋₆ alkynyl group substituted by a phenylgroup (provided that such a phenyl group may be substituted by one ormore substituents selected from the group consisting of a halogen atom,a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl groupsubstituted by a phenoxy group (provided that such a phenoxy group maybe substituted by one or more substituents selected from the groupconsisting of a halogen atom, a trifluoromethyl group, a nitro group, aC₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),a C₁₋₆ alkyl group substituted by a phenylthio group (provided that sucha phenylthio group may be substituted by one or more substituentsselected from the group consisting of a halogen atom, a trifluoromethylgroup, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by aphenylsulfinyl group (provided that such a phenylsulfinyl group may besubstituted by one or more substituents selected from the groupconsisting of a halogen atom, a trifluoromethyl group, a nitro group, aC₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),a C₁₋₆ alkyl group substituted by a phenylsulfonyl group (provided thatsuch a phenylsulfonyl group may be substituted by one or moresubstituents selected from the group consisting of a halogen atom, atrifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxygroup and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substitutedby a benzyloxy group (provided that the phenyl group of such a benzyloxygroup may be substituted by one or more substituents selected from thegroup consisting of a halogen atom, a trifluoromethyl group, a nitrogroup, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonylgroup), a C₁₋₆ alkyl group substituted by a benzylthio group (providedthat the phenyl group of such a benzylthio group may be substituted byone or more substituents selected from the group consisting of a halogenatom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl groupsubstituted by a benzylsulfinyl group (provided that the phenyl group ofsuch a benzylsulfinyl group may be substituted by one or moresubstituents selected from the group consisting of a halogen atom, atrifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxygroup and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substitutedby a benzylsulfonyl group (provided that the phenyl group of such abenzylsulfonyl group may be substituted by one or more substituentsselected from the group consisting of a halogen atom, a trifluoromethylgroup, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by aphenylcarbonyl group (provided that such a phenylcarbonyl group may besubstituted by one or more substituents selected from the groupconsisting of a halogen atom, a trifluoromethyl group, a nitro group, aC₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),a C₁₋₆ alkyl group substituted by a benzylcarbonyl group (provided thatthe phenyl group of such a benzylcarbonyl group may be substituted byone or more substituents selected from the group consisting of a halogenatom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl groupsubstituted by an amino group substituted by a C₁₋₄ alkylsulfonyl group,or a C₁₋₆ alkyl group substituted by an amino group substituted by aC₂₋₄ alkylcarbonyl group, each of R^(d2), R^(d3) and R^(d4) which areindependent of one another, is a hydrogen atom, a C₁₋₈ alkyl group, aC₂₋₈ alkenyl group, a C₂₋₈ alkynyl group, or a phenyl group (providedthat such a phenyl group may be substituted by one or more substituentsselected from the group consisting of a halogen atom, a trifluoromethylgroup, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), R^(d5) is a C₁₋₈ alkyl group, a C₂₋₈ alkenylgroup, a C₂₋₈ alkynyl group, or a phenyl group (provided that such aphenyl group may be substituted by one or more substituents selectedfrom the group consisting of a halogen atom, a trifluoromethyl group, anitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), R^(d6) is a C₁₋₈ alkyl group, a C₂₋₈ alkenylgroup, a C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆alkylthio group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfinylgroup, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfonyl group, aC₁₋₆ alkyl group substituted by a C₁₋₆ alkoxy group, a C₁₋₆ alkyl groupsubstituted by a C₂₋₇ alkoxycarbonyl group, a C₁₋₆ alkyl groupsubstituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl groupsubstituted by a cyano group, a phenyl group (provided that such aphenyl group may be substituted by one or more substituents selectedfrom the group consisting of a halogen atom, a trifluoromethyl group, anitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), or a C₁₋₆ alkyl group substituted by a phenylgroup (provided that such a phenyl group may be substituted by one ormore substituents selected from the group consisting of a halogen atom,a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆alkoxy group and a C₂₋₇ alkoxycarbonyl group), R^(f1) is a C₁₋₈ alkylgroup, a C₃₋₇ cycloalkyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇cycloalkyl group, a C₃₋₇ cycloalkenyl group, a C₁₋₆ alkyl groupsubstituted by a C₃₋₇ cycloalkenyl group, a C₂₋₈ alkenyl group, a C₂₋₈alkynyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxy group, aC₁₋₆ alkyl group substituted by a C₂₋₆ alkenyloxy group, a C₁₋₆ alkylgroup substituted by a C₂₋₆ alkynyloxy group, a C₁₋₆ alkyl groupsubstituted by a mono-, di- or poly-halogeno C₁₋₆ alkoxy group, a C₁₋₆alkyl group substituted by a mono-, di- or poly-halogeno C₂₋₆ alkenyloxygroup, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogenoC₂₋₆ alkynyloxy group, a C₁₋₆ alkyl group substituted by a C₁₋₆alkylthio group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfinylgroup, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfonyl group, amono-, di- or poly-halogeno C₁₋₈ alkyl group, a mono-, di- orpoly-halogeno C₂₋₈ alkenyl group, a mono-, di- or poly-halogeno C₂₋₈alkynyl group, a C₁₋₆ alkyl group substituted by a cyano group, a C₂₋₆alkenyl group substituted by a cyano group, a C₂₋₆ alkynyl groupsubstituted by a cyano group, a C₁₋₆ alkyl group substituted by a nitrogroup, a C₂₋₆ alkenyl group substituted by a nitro group, a C₂₋₆ alkynylgroup substituted by a nitro group, a C₁₋₆ alkyl group substituted by aC₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkenyl group substituted by a C₂₋₇alkoxycarbonyl group, a C₂₋₆ alkynyl group substituted by a C₂₋₇alkoxycarbonyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a mono-, di- orpoly-halogeno C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substitutedby a C₃₋₇ alkenylcarbonyl group, a C₁₋₆ alkyl group substituted by aC₃₋₇ alkynylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₂₋₅alkylcarbonyl group substituted by a C₁₋₄ alkoxy group, a C₁₋₆ alkylgroup substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄alkylthio group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonylgroup substituted by a C₁₋₄ alkylsulfinyl group, a C₁₋₆ alkyl groupsubstituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄alkylsulfonyl group, a C₂₋₆ alkenyl group substituted by a C₂₋₇alkylcarbonyl group, a C₂₋₆ alkynyl group substituted by a C₂₋₇alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆alkylsulfamoyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆alkoxysulfamoyl group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃alkyl)sulfamoyl group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃alkyl)-N-(C₁₋₃ alkoxy)sulfamoyl group, a C₁₋₆ alkyl group substituted bya C₂₋₇ alkylcarbamoyl group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃alkyl)carbamoyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇alkoxycarbamoyl group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃alkyl)-N-(C₁₋₃ alkoxy)carbamoyl group, a C₁₋₆ alkyl group substituted bya C₁₋₆ alkylamino group, a C₁₋₆ alkyl group substituted by a C₁₋₆alkoxyamino group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃alkyl)-N-(C₁₋₃ alkoxy)amino group, a C₁₋₆ alkyl group substituted by anN-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆ alkyl)amino group, a C₁₋₆ alkyl groupsubstituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆ alkoxy)amino group, aC₁₋₆ alkyl group substituted by an N-(C₁₋₆ alkylsulfonyl)-N-(C₁₋₆alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₆alkylsulfonyl)-N-(C₁₋₆ alkoxy)amino group, a phenyl group (provided thatsuch a phenyl group may be substituted by one or more substituentsselected from the group consisting of a halogen atom, a trifluoromethylgroup, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenyl group(provided that such a phenyl group may be substituted by one or moresubstituents selected from the group consisting of a halogen atom, atrifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxygroup and a C₂₋₇ alkoxycarbonyl group), a C₂₋₇ alkenyl group substitutedby a phenyl group (provided that such a phenyl group may be substitutedby one or more substituents selected from the group consisting of ahalogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkylgroup, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₂₋₆alkynyl group substituted by a phenyl group (provided that such a phenylgroup may be substituted by one or more substituents selected from thegroup consisting of a halogen atom, a trifluoromethyl group, a nitrogroup, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonylgroup), a C₁₋₆ alkyl group substituted by a phenoxy group (provided thatsuch a phenoxy group may be substituted by one or more substituentsselected from the group consisting of a halogen atom, a trifluoromethylgroup, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylthiogroup (provided that such a phenylthio group may be substituted by oneor more substituents selected from the group consisting of a halogenatom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl groupsubstituted by a phenylsulfinyl group (provided that such aphenylsulfinyl group may be substituted by one or more substituentsselected from the group consisting of a halogen atom, a trifluoromethylgroup, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by aphenylsulfonyl group (provided that such a phenylsulfonyl group may besubstituted by one or more substituents selected from the groupconsisting of a halogen atom, a trifluoromethyl group, a nitro group, aC₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),a C₁₋₆ alkyl group substituted by a benzyloxy group (provided that thephenyl group of such a benzyloxy group may be substituted by one or moresubstituents selected from the group consisting of a halogen atom, atrifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxygroup and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substitutedby a benzylthio group (provided that the phenyl group of such abenzylthio group may be substituted by one or more substituents selectedfrom the group consisting of a halogen atom, a trifluoromethyl group, anitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by abenzylsulfinyl group (provided that the phenyl group of such abenzylsulfinyl group may be substituted by one or more substituentsselected from the group consisting of a halogen atom, a trifluoromethylgroup, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by abenzylsulfonyl group (provided that the phenyl group of such abenzylsulfonyl group may be substituted by one or more substituentsselected from the group consisting of a halogen atom, a trifluoromethylgroup, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by aphenylcarbonyl group (provided that such a phenylcarbonyl group may besubstituted by one or more substituents selected from the groupconsisting of a halogen atom, a trifluoromethyl group, a nitro group, aC₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),a C₁₋₆ alkyl group substituted by a benzylcarbonyl group (provided thatthe phenyl group of such a benzylcarbonyl group may be substituted byone or more substituents selected from the group consisting of a halogenatom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl groupsubstituted by an amino group substituted by a C₁₋₄ alkylsulfonyl group,or a C₁₋₆ alkyl group substituted by an amino group substituted by aC₂₋₄ alkylcarbonyl group, R^(f2) is a C₁₋₈ alkyl group, a C₂₋₈ alkenylgroup, a C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆alkylthio group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfinylgroup, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfonyl group, aC₁₋₆ alkyl group substituted by a C₁₋₆ alkoxy group, a C₁₋₆ alkyl groupsubstituted by a C₂₋₇ alkoxycarbonyl group, a C₁₋₆ alkyl groupsubstituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl groupsubstituted by a cyano group, a phenyl group (provided that such aphenyl group may be substituted by one or more substituents selectedfrom the group consisting of a halogen atom, a trifluoromethyl group, anitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), or a C₁₋₆ alkyl group substituted by a phenylgroup (provided that such a phenyl group may be substituted by one ormore substituents selected from the group consisting of a halogen atom,a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆alkoxy group and a C₂₋₇ alkoxycarbonyl group), each of R^(f3) and R^(f4)which are independent of one another, is a hydrogen atom, a C₁₋₆ alkylgroup, a mono-, di- or poly-halogeno C₁₋₆ alkyl group, a C₁₋₆ alkoxygroup, a mono-, di- or poly-halogeno C₁₋₆ alkoxy group, a C₁₋₆ alkylthiogroup, a C₁₋₆ alkylsulfinyl group, a C₁₋₆ alkylsulfonyl group, a C₂₋₇alkoxycarbonyl group, a C₂₋₇ alkylcarbonyl group, a halogen atom, anitro group, a cyano group, or a phenyl group (provided that such aphenyl group may be substituted by one or more substituents selectedfrom the group consisting of a halogen atom, a trifluoromethyl group, anitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), each of R^(f5) and R^(f6) which are independentof one another, is a hydrogen atom, a C₁₋₈ alkyl group, a C₂₋₈ alkenylgroup, a C₂₋₈ alkynyl group, or a phenyl group (provided that such aphenyl group may be substituted by one or more substituents selectedfrom the group consisting of a halogen atom, a trifluoromethyl group, anitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇alkoxycarbonyl group), X is an oxygen atom or a sulfur atom, L is ahydrogen atom, a C₁₋₆ alkyl group, a C₂₋₆ alkenyl group or a C₂₋₆alkynyl group, G is ##STR789## A is a CH group and each of γ and D whichare independent of each other, is a C₁₋₄ alkyl group, a C₁₋₄ alkoxygroup, a mono-, di- or poly-halogeno C₁₋₄ alkyl group, a mono-, di- orpoly-halogeno C₁₋₄ alkoxy group, a halogen atom, a C₁₋₄ alkylaminogroup, or a di(C₁₋₄ alkyl)amino group.
 2. The iminosulfonylureaderivative or its salt according to claim 1, wherein Q is ##STR790## 3.The iminosulfonylurea derivative or its salt according to claim 1,wherein Q is ##STR791##
 4. The iminosulfonylurea derivative or its saltaccording to claim 1, wherein Q is ##STR792##
 5. The iminosulfonylureaderivative or its salt according to claim 1, wherein Q is ##STR793## 6.The iminosulfonylurea derivative or its salt according to claim 1,wherein Q is ##STR794##
 7. A herbicidal and growth control methodagainst weeds, which comprises applying a herbicidally effective amountof an iminosulfonylurea derivative defined in claim
 1. 8. A herbicidaland growth control method against weeds, which comprises applying aherbicidally effective amount of an iminosulfonylurea derivative definedin claim
 2. 9. A herbicidal and growth control method against weeds,which comprises applying a herbicidally effective amount of animinosulfonylurea derivative defined in claim
 3. 10. A herbicidal andgrowth control method against weeds, which comprises applying aherbicidally effective amount of an iminosulfonylurea derivative definedin claim
 4. 11. A herbicidal and growth control method against weeds,which comprises applying a herbicidally effective amount of animinosulfonylurea derivative defined in claim
 5. 12. A herbicidal andgrowth control method against weeds, which comprises applying aherbicidally effective amount of an iminosulfonylurea derivative definedin claim
 6. 13. A herbicidal composition comprising an effective amountof a compound of the formula (I) as described in claim 1 and an inertcarrier.
 14. The herbicidal composition of claim 13 wherein Q, in saidcompound of the formula (I), is ##STR795##
 15. The herbicidalcomposition of claim 13 wherein Q, in said compound of the formula (I),is ##STR796##
 16. The herbicidal composition of claim 13 wherein Q, insaid compound of the formula (I), is ##STR797##
 17. The herbicidalcomposition of claim 13 wherein Q, in said compound of the formula (I),is ##STR798##
 18. The herbicidal composition of claim 13 wherein Q, insaid compound of the formula (I), is ##STR799##